Hasan Yakan, M. Azam, S. Kansız, H. Muğlu, M. Ergül, Parham Taslimi, Ümit M. Koçyiğit, M. Karaman, Saud I. Al-Resayes, Kim Min
ABSTRACT. We are reporting a novel series of thiosemicarbazone derivatives derived from isatin (1-6), structural determination, and investigation of the inhibitory properties against proliferative, carbonic anhydrase, and cholinesterase enzymes. The anti-proliferative effects of the compounds were measured by XTT assay against MCF-7 and MDA-MB-231 cancerous cell lines. Compound 3 showed significant cytotoxic effects on both MCF-7 and MDA-MB-231 cell lines, with IC50 values of 8.19 μM and 23.41 μM, respectively. In addition, the compounds (1-6) inhibited the hCA I and II, their Ki values 2.01 ± 0.35 – 21.55 ± 2.56 and 1.24 ± 0.33 – 25.03 ± 5.48 µM, respectively. AChE was also successfully inhibited by these compounds (1-6), with Ki values ranging from 40.37 ± 8.23 to 125.43 ± 24.93 µM. The best Ki values for 3, 6, and 4 for α-glycosidase were 564.35 ± 72.06, 594.38 ± 52.04, and 683.437 ± 66.58 µM, respectively. Binding affinities were determined to be -6.697 kcal/mol, -8.251 kcal/mol, -9.932 kcal/mol, and -4.946 kcal/mol for hCA I, hCA II, AChE, and α-glucosidase enzymes, respectively. These findings reveal that the formed compounds containing isatin moieties were crucial in the enzyme inhibition. KEY WORDS: Isatin, Thiosemicarbazone, Anti-proliferative activity, Enzyme inhibition, Molecular docking Bull. Chem. Soc. Ethiop. 2023, 37(5), 1221-1236. DOI: https://dx.doi.org/10.4314/bcse.v37i5.14
{"title":"Isatin/thiosemicarbohydrazone hybrids: Facile synthesis, and their evaluation as anti-proliferatıve agents and metabolıc enzyme inhibitors","authors":"Hasan Yakan, M. Azam, S. Kansız, H. Muğlu, M. Ergül, Parham Taslimi, Ümit M. Koçyiğit, M. Karaman, Saud I. Al-Resayes, Kim Min","doi":"10.4314/bcse.v37i5.14","DOIUrl":"https://doi.org/10.4314/bcse.v37i5.14","url":null,"abstract":"ABSTRACT. We are reporting a novel series of thiosemicarbazone derivatives derived from isatin (1-6), structural determination, and investigation of the inhibitory properties against proliferative, carbonic anhydrase, and cholinesterase enzymes. The anti-proliferative effects of the compounds were measured by XTT assay against MCF-7 and MDA-MB-231 cancerous cell lines. Compound 3 showed significant cytotoxic effects on both MCF-7 and MDA-MB-231 cell lines, with IC50 values of 8.19 μM and 23.41 μM, respectively. In addition, the compounds (1-6) inhibited the hCA I and II, their Ki values 2.01 ± 0.35 – 21.55 ± 2.56 and 1.24 ± 0.33 – 25.03 ± 5.48 µM, respectively. AChE was also successfully inhibited by these compounds (1-6), with Ki values ranging from 40.37 ± 8.23 to 125.43 ± 24.93 µM. The best Ki values for 3, 6, and 4 for α-glycosidase were 564.35 ± 72.06, 594.38 ± 52.04, and 683.437 ± 66.58 µM, respectively. Binding affinities were determined to be -6.697 kcal/mol, -8.251 kcal/mol, -9.932 kcal/mol, and -4.946 kcal/mol for hCA I, hCA II, AChE, and α-glucosidase enzymes, respectively. These findings reveal that the formed compounds containing isatin moieties were crucial in the enzyme inhibition. \u0000 \u0000KEY WORDS: Isatin, Thiosemicarbazone, Anti-proliferative activity, Enzyme inhibition, Molecular docking \u0000 \u0000Bull. Chem. Soc. Ethiop. 2023, 37(5), 1221-1236. \u0000DOI: https://dx.doi.org/10.4314/bcse.v37i5.14","PeriodicalId":9501,"journal":{"name":"Bulletin of the Chemical Society of Ethiopia","volume":" ","pages":""},"PeriodicalIF":1.2,"publicationDate":"2023-07-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47181192","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Amal H. Al-Bagawi, Ragaa El Sheikh, Osama M.A. Salem, Ghada M. Abdel Fattah, Mohannad M. Garoub, Ayman A. Gouda
ABSTRACT. For acyclovir (ACV) determination in bulk and dosage forms, quick, sensitive, straightforward, and eco-friendly ultrasound-assisted dispersive liquid-liquid microextraction (UA-DLLME)-based spectrophotometric method has been created and validated. ACV with 1,2-naphthoquine-4-sulfonate (NQS) react in alkaline medium to produce a yellow-colored product, which is the basis of the newly created method. Investigation and optimization were done on the crucial experimental variables influencing ACV's extraction effectiveness. At λmax = 495 nm, the minuscule organic droplets were detected. The linearity was present from 0.1 to 3.0 μg/mL under ideal circumstances, with a linear correlation coefficient of 0.9995. The detection limit was 0.03 μg/mL and quantification limit was 0.1 μg/mL. 22.50 was the enrichment factor. Relative standard deviation (RSD%) as accuracy at 2.0 μg/mL of ACV was 1.0%, with good recovery (99.30%). The developed UA-DLLME method was effectively used to determine the ACV in dosage forms, and the validation was evaluated. Results from the suggested technique for dosage forms and pure ACV were in excellent agreement with the results from the official method. KEY WORDS: Ultrasound-assissted, Dispersive liquid–liquid microextraction, Acyclovir, Spectrophotometry, Dosage forms Bull. Chem. Soc. Ethiop. 2023, 37(5), 1081-1092. DOI: https://dx.doi.org/10.4314/bcse.v37i5.2
{"title":"Ultrasound-assisted dispersive liquid-liquid microextraction approach for preconcentration of acyclovir as antiviral drug in dosage forms prior to spectrophotometric determination","authors":"Amal H. Al-Bagawi, Ragaa El Sheikh, Osama M.A. Salem, Ghada M. Abdel Fattah, Mohannad M. Garoub, Ayman A. Gouda","doi":"10.4314/bcse.v37i5.2","DOIUrl":"https://doi.org/10.4314/bcse.v37i5.2","url":null,"abstract":"ABSTRACT. For acyclovir (ACV) determination in bulk and dosage forms, quick, sensitive, straightforward, and eco-friendly ultrasound-assisted dispersive liquid-liquid microextraction (UA-DLLME)-based spectrophotometric method has been created and validated. ACV with 1,2-naphthoquine-4-sulfonate (NQS) react in alkaline medium to produce a yellow-colored product, which is the basis of the newly created method. Investigation and optimization were done on the crucial experimental variables influencing ACV's extraction effectiveness. At λmax = 495 nm, the minuscule organic droplets were detected. The linearity was present from 0.1 to 3.0 μg/mL under ideal circumstances, with a linear correlation coefficient of 0.9995. The detection limit was 0.03 μg/mL and quantification limit was 0.1 μg/mL. 22.50 was the enrichment factor. Relative standard deviation (RSD%) as accuracy at 2.0 μg/mL of ACV was 1.0%, with good recovery (99.30%). The developed UA-DLLME method was effectively used to determine the ACV in dosage forms, and the validation was evaluated. Results from the suggested technique for dosage forms and pure ACV were in excellent agreement with the results from the official method. \u0000 \u0000KEY WORDS: Ultrasound-assissted, Dispersive liquid–liquid microextraction, Acyclovir, Spectrophotometry, Dosage forms \u0000Bull. Chem. Soc. Ethiop. 2023, 37(5), 1081-1092. \u0000DOI: https://dx.doi.org/10.4314/bcse.v37i5.2","PeriodicalId":9501,"journal":{"name":"Bulletin of the Chemical Society of Ethiopia","volume":" ","pages":""},"PeriodicalIF":1.2,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45076783","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ABSTRACT. Heterocyclic pyridazine continues to attract great interest, mainly arising from a large variety of interesting pharmacological activities, herbicides, insecticides, and fungicides. On the other hand, the current interest in selenium-containing heterocycles is a result of their chemical properties and biological activities. In addition to the many recent publications dealing with the pharmacological potential of a selenium compound, new active formulations are an attractive target for chemical research. 2-((3-cyano-4,6-dimethylpyridin-2-yl)selanyl) acetic acid (pyd-Se), 2-((4-cyano-5,6-diphenylpyridazin-3-yl)selanyl)acetic acid (pydz-Se) and 2-((4,6-dimethyl quinolin-2-yl)selanyl)acetic acid (quin-Se) reacts with gold(III) chloride to produce metal ion complexes of specific composition. These synthesized complexes were characterized by elemental analyses, molar conductivity, FTIR, 1H NMR and transmission electron microscopy (TEM) investigations. The complexes were found to have the formulas [Au(pyd-Se)2]Cl, [Au(pydz-Se)2]Cl and Au(quin-Se)2]Cl, respectively.
KEY WORDS: Au(III), Organoselenium, Complexation, FTIR, 1H NMR, TEM
Bull. Chem. Soc. Ethiop. 2023, 37(5), 1141-1150.
DOI: https://dx.doi.org/10.4314/bcse.v37i5.7
{"title":"Synthesis and spectroscopic investigations of Au(III) seleno-organic complexes","authors":"Shams H. Abdel-Hafez, Moamen S. Refat","doi":"10.4314/bcse.v37i5.7","DOIUrl":"https://doi.org/10.4314/bcse.v37i5.7","url":null,"abstract":"ABSTRACT. Heterocyclic pyridazine continues to attract great interest, mainly arising from a large variety of interesting pharmacological activities, herbicides, insecticides, and fungicides. On the other hand, the current interest in selenium-containing heterocycles is a result of their chemical properties and biological activities. In addition to the many recent publications dealing with the pharmacological potential of a selenium compound, new active formulations are an attractive target for chemical research. 2-((3-cyano-4,6-dimethylpyridin-2-yl)selanyl) acetic acid (pyd-Se), 2-((4-cyano-5,6-diphenylpyridazin-3-yl)selanyl)acetic acid (pydz-Se) and 2-((4,6-dimethyl quinolin-2-yl)selanyl)acetic acid (quin-Se) reacts with gold(III) chloride to produce metal ion complexes of specific composition. These synthesized complexes were characterized by elemental analyses, molar conductivity, FTIR, 1H NMR and transmission electron microscopy (TEM) investigations. The complexes were found to have the formulas [Au(pyd-Se)2]Cl, [Au(pydz-Se)2]Cl and Au(quin-Se)2]Cl, respectively.
 
 KEY WORDS: Au(III), Organoselenium, Complexation, FTIR, 1H NMR, TEM
 Bull. Chem. Soc. Ethiop. 2023, 37(5), 1141-1150. 
 DOI: https://dx.doi.org/10.4314/bcse.v37i5.7","PeriodicalId":9501,"journal":{"name":"Bulletin of the Chemical Society of Ethiopia","volume":"12 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"136300403","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
G. Puthilibai, V. Devatarika, Byeon Haewon, Shyam Sundar Behura, Hitendra Kumar Lautre, V. Subha, P. Sangwan, J. Sunil
ABSTRACT. Metal complexes play an important role in agriculture, pharmacology, medicine, and industrial chemistry. Schiff base metal compounds are the fusion products of propene and aldehydes, require a metal surrounded by an ion or cluster of molecules to form. Metal complexes of Co(II), Ni(II), Cu(II), and Zn(II) have also been created. Elemental analysis is used to analyses the structure and related compounds of the produced Schiff base ligand. According to deoxyribose nucleic acid (DNA) binding tests, Schiff base metal(II) complexes attach to DNA in an intercalative form with weak covalent connections. The predicted DNA binding mode supports an increase in the complexes' binding activity in the presence of newly generated ligand. The cleavage activities of the DNA were recorded using gel-electrophoresis in the presence and absence of the complexes. The findings of the cleavage experiment show that all of the produced chelates can successfully cut DNA. KEY WORDS: Schiff base ligand, DNA, Metal(II) complex, Hetero-ligand cobalt(II), Aldehydes Bull. Chem. Soc. Ethiop. 2023, 37(5), 1133-1139. DOI: https://dx.doi.org/10.4314/bcse.v37i5.6
{"title":"Synthesized and hypothesized schiff base ligand and its metal(II) complexes DNA binding mode","authors":"G. Puthilibai, V. Devatarika, Byeon Haewon, Shyam Sundar Behura, Hitendra Kumar Lautre, V. Subha, P. Sangwan, J. Sunil","doi":"10.4314/bcse.v37i5.6","DOIUrl":"https://doi.org/10.4314/bcse.v37i5.6","url":null,"abstract":"ABSTRACT. Metal complexes play an important role in agriculture, pharmacology, medicine, and industrial chemistry. Schiff base metal compounds are the fusion products of propene and aldehydes, require a metal surrounded by an ion or cluster of molecules to form. Metal complexes of Co(II), Ni(II), Cu(II), and Zn(II) have also been created. Elemental analysis is used to analyses the structure and related compounds of the produced Schiff base ligand. According to deoxyribose nucleic acid (DNA) binding tests, Schiff base metal(II) complexes attach to DNA in an intercalative form with weak covalent connections. The predicted DNA binding mode supports an increase in the complexes' binding activity in the presence of newly generated ligand. The cleavage activities of the DNA were recorded using gel-electrophoresis in the presence and absence of the complexes. The findings of the cleavage experiment show that all of the produced chelates can successfully cut DNA. \u0000 \u0000KEY WORDS: Schiff base ligand, DNA, Metal(II) complex, Hetero-ligand cobalt(II), Aldehydes \u0000Bull. Chem. Soc. Ethiop. 2023, 37(5), 1133-1139. \u0000DOI: https://dx.doi.org/10.4314/bcse.v37i5.6","PeriodicalId":9501,"journal":{"name":"Bulletin of the Chemical Society of Ethiopia","volume":" ","pages":""},"PeriodicalIF":1.2,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46115723","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
ABSTRACT. Cancer is one of the most deadly diseases worldwide, challenging the world for effective treatment of the diseases, to tackle this problem a vast amount of therapeutic candidates are being investigated. Indole-benzimidazole structures have recently gained considerable attention, because compounds containing these structure exhibit a very good anticancer property. Two series of novel indole-benzimidazole hybrids molecules viz., 2-(5-substituted-1H-indol-3-yl)-5-substituted-1H-benzo[d]imidazole 5(a-f) and 2-(5-substituted-1-(3-methylbut-2-enyl)-1H-indol-3-yl)-5-substituted-1H-benzo[d]imidazole 6(a-f) were synthesized and characterized by spectroscopic techniques. The twelve target molecules have been investigated for their in-vitro cytotoxic activity against human ovarian carcinoma cells (SKOV-3), human prostate cancer cells (PC-3), human cervical cancer cells (HeLa) and human acute monocytic leukemia cells (THP-1) using MTT assay. Compound; 2-(5-bromo-1H-indol-3-yl)-5-methyl-1H-benzo[d]imidazole (5e) was interesting with IC50 (μM) values of 23.69 (SKOV-3), 73.05 (PC-3), 64.66 (HeLa) and 39.08 (THP-1), respectively. KEY WORDS: Indole, Benzimidazole, Hybrid molecules, Anticancer activity Bull. Chem. Soc. Ethiop. 2023, 37(5), 1209-1220. DOI: https://dx.doi.org/10.4314/bcse.v37i5.13
{"title":"Design and synthesis of indole-benzimidazole hybrid molecules and evaluation of their in-vitro cytotoxic activities","authors":"S. Hamza, Sherif, Y. Murthy*","doi":"10.4314/bcse.v37i5.13","DOIUrl":"https://doi.org/10.4314/bcse.v37i5.13","url":null,"abstract":"ABSTRACT. Cancer is one of the most deadly diseases worldwide, challenging the world for effective treatment of the diseases, to tackle this problem a vast amount of therapeutic candidates are being investigated. Indole-benzimidazole structures have recently gained considerable attention, because compounds containing these structure exhibit a very good anticancer property. Two series of novel indole-benzimidazole hybrids molecules viz., 2-(5-substituted-1H-indol-3-yl)-5-substituted-1H-benzo[d]imidazole 5(a-f) and 2-(5-substituted-1-(3-methylbut-2-enyl)-1H-indol-3-yl)-5-substituted-1H-benzo[d]imidazole 6(a-f) were synthesized and characterized by spectroscopic techniques. The twelve target molecules have been investigated for their in-vitro cytotoxic activity against human ovarian carcinoma cells (SKOV-3), human prostate cancer cells (PC-3), human cervical cancer cells (HeLa) and human acute monocytic leukemia cells (THP-1) using MTT assay. Compound; 2-(5-bromo-1H-indol-3-yl)-5-methyl-1H-benzo[d]imidazole (5e) was interesting with IC50 (μM) values of 23.69 (SKOV-3), 73.05 (PC-3), 64.66 (HeLa) and 39.08 (THP-1), respectively. \u0000 \u0000KEY WORDS: Indole, Benzimidazole, Hybrid molecules, Anticancer activity \u0000 \u0000Bull. Chem. Soc. Ethiop. 2023, 37(5), 1209-1220. \u0000DOI: https://dx.doi.org/10.4314/bcse.v37i5.13 ","PeriodicalId":9501,"journal":{"name":"Bulletin of the Chemical Society of Ethiopia","volume":" ","pages":""},"PeriodicalIF":1.2,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"43914962","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Bereket Tesfaye, Tsegaye Girma Asere, Guyo Jilo Molole, A. Gure
ABSTRACT. In this paper, effervescence-assisted dispersive liquid-liquid microextraction method has been developed for the extraction and preconcentration of organochlorine pesticides in water samples before their determination by gas chromatography-mass spectrometry. The method involves in-situ generation of CO2 bubbles to induce dispersion of the extraction solvent in the aqueous sample. Different parameters affecting the extraction efficiency of the method including the type and concentration of the effervescent agents as well as the type and volume of extraction solvent were optimized. Under optimum conditions, matrix matched calibration curves were constructed at eight concentrations ranging from 0.6–4.0 ng/mL showed good linearity with coefficient of determinations of ≥ 0.9961. The limits of detections and quantifications ranged from 0.2–0.4 and 0.6–1.0 ng/mL, respectively. The intra- and inter-day precisions studied at two concentration levels had below 5% relative standard deviation values. Similarly, recoveries investigated at two concentration levels ranged from 80.7–117.4%. The findings demonstrated that proposed method is simple, rapid, and efficient to be used as alternative method for analysis of organochlorine pesticides from environmental water and other similar matrices. KEY WORDS: Effervescence agents, CO2 bubbles, Organochlorine pesticides, Water samples, gas chromatography-mass spectroscopy Bull. Chem. Soc. Ethiop. 2023, 37(5), 1109-1122. DOI: https://dx.doi.org/10.4314/bcse.v37i5.4
{"title":"Effervescence-assisted dispersive liquid-liquid microextraction for extraction and preconcentration of organochlorine pesticides in water samples","authors":"Bereket Tesfaye, Tsegaye Girma Asere, Guyo Jilo Molole, A. Gure","doi":"10.4314/bcse.v37i5.4","DOIUrl":"https://doi.org/10.4314/bcse.v37i5.4","url":null,"abstract":"ABSTRACT. In this paper, effervescence-assisted dispersive liquid-liquid microextraction method has been developed for the extraction and preconcentration of organochlorine pesticides in water samples before their determination by gas chromatography-mass spectrometry. The method involves in-situ generation of CO2 bubbles to induce dispersion of the extraction solvent in the aqueous sample. Different parameters affecting the extraction efficiency of the method including the type and concentration of the effervescent agents as well as the type and volume of extraction solvent were optimized. Under optimum conditions, matrix matched calibration curves were constructed at eight concentrations ranging from 0.6–4.0 ng/mL showed good linearity with coefficient of determinations of ≥ 0.9961. The limits of detections and quantifications ranged from 0.2–0.4 and 0.6–1.0 ng/mL, respectively. The intra- and inter-day precisions studied at two concentration levels had below 5% relative standard deviation values. Similarly, recoveries investigated at two concentration levels ranged from 80.7–117.4%. The findings demonstrated that proposed method is simple, rapid, and efficient to be used as alternative method for analysis of organochlorine pesticides from environmental water and other similar matrices. \u0000 \u0000KEY WORDS: Effervescence agents, CO2 bubbles, Organochlorine pesticides, Water samples, gas chromatography-mass spectroscopy \u0000 \u0000Bull. Chem. Soc. Ethiop. 2023, 37(5), 1109-1122. \u0000DOI: https://dx.doi.org/10.4314/bcse.v37i5.4 ","PeriodicalId":9501,"journal":{"name":"Bulletin of the Chemical Society of Ethiopia","volume":" ","pages":""},"PeriodicalIF":1.2,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47640025","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Ruiji Li, Q. Fang, Bingzhao Mou, Minghui Chen, Qiwen Tang, B. Shen, Dong Wang, Wei Li
ABSTRACT. A compound S,S-bis(2-(prop-1-yn-1-yl)phenyl) ethanebis(thioate) is synthesized through one-pot synthesis. The lithiation reaction of 3-bromo-2-methylbenzo[b]thiophene by using n-butyllithium, is followed by conversion to the corresponding organocopper compound, and subsequent reaction with oxalyl chloride to afford the target compound. The chemical structure of the final compound is well confirmed by NMR, HRMS and X-ray analysis. Meanwhile, the proposed reaction mechanism is fully discussed. Furthermore, the chemiluminescent reaction by using target compound to release light is also investigated. This work provides a convenient synthetic approach for obtaining S,S-diphenyl ethanebis(thioate) compound and broadening its application in chemiluminescence. KEY WORDS: One pot synthesis, S,S-Diphenyl ethanebis(thioate) compound, Crystal structure, Reaction mechanism, Chemiluminescence Bull. Chem. Soc. Ethiop. 2023, 37(5), 1185-1191. DOI: https://dx.doi.org/10.4314/bcse.v37i5.11
{"title":"A convenient one pot synthesis, crystal structure and chemiluminescence of S,S-diphenyl ethanebis(thioate) compound","authors":"Ruiji Li, Q. Fang, Bingzhao Mou, Minghui Chen, Qiwen Tang, B. Shen, Dong Wang, Wei Li","doi":"10.4314/bcse.v37i5.11","DOIUrl":"https://doi.org/10.4314/bcse.v37i5.11","url":null,"abstract":"ABSTRACT. A compound S,S-bis(2-(prop-1-yn-1-yl)phenyl) ethanebis(thioate) is synthesized through one-pot synthesis. The lithiation reaction of 3-bromo-2-methylbenzo[b]thiophene by using n-butyllithium, is followed by conversion to the corresponding organocopper compound, and subsequent reaction with oxalyl chloride to afford the target compound. The chemical structure of the final compound is well confirmed by NMR, HRMS and X-ray analysis. Meanwhile, the proposed reaction mechanism is fully discussed. Furthermore, the chemiluminescent reaction by using target compound to release light is also investigated. This work provides a convenient synthetic approach for obtaining S,S-diphenyl ethanebis(thioate) compound and broadening its application in chemiluminescence. \u0000 \u0000KEY WORDS: One pot synthesis, S,S-Diphenyl ethanebis(thioate) compound, Crystal structure, Reaction mechanism, Chemiluminescence \u0000Bull. Chem. Soc. Ethiop. 2023, 37(5), 1185-1191. \u0000DOI: https://dx.doi.org/10.4314/bcse.v37i5.11","PeriodicalId":9501,"journal":{"name":"Bulletin of the Chemical Society of Ethiopia","volume":" ","pages":""},"PeriodicalIF":1.2,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46109900","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Dhekra Jawad Hashim, Eman H. Al-Rikabi, Angham G. Hadi, Sadiq J. Baqir
ABSTRACT. 4-Aminoantipyrine was used as ligand to prepare new complexes of triphenyltin, di-butyl and dimethyl-tin complexes by condensation reaction with the corresponding organotin chloride salts. The complexes were identified by different techniques, such as infrared spectra, (tin and proton) magnetic resonance and elemental analyses. The antioxidant activity of 4-aminoantipyrine and prepared complexes were studied by two different methods; Free radical scavenging activity DPPH and CUPRRAC methods. Tri and di-tin complexes gave high percentage inhibition than ligand with both methods due to tin moiety, also triphenyltin carboxylate complex was the best compared with the others. KEY WORDS: 4-Aminoantipyrine, Condensation, Triphenyl tin chloride, DPPH and CUPRRAC methods Bull. Chem. Soc. Ethiop. 2023, 37(5), 1163-1170. DOI: https://dx.doi.org/10.4314/bcse.v37i5.9
{"title":"4-Aminoantipyrine-new organotin complexes, synthesis, structure and antioxidant activity","authors":"Dhekra Jawad Hashim, Eman H. Al-Rikabi, Angham G. Hadi, Sadiq J. Baqir","doi":"10.4314/bcse.v37i5.9","DOIUrl":"https://doi.org/10.4314/bcse.v37i5.9","url":null,"abstract":"ABSTRACT. 4-Aminoantipyrine was used as ligand to prepare new complexes of triphenyltin, di-butyl and dimethyl-tin complexes by condensation reaction with the corresponding organotin chloride salts. The complexes were identified by different techniques, such as infrared spectra, (tin and proton) magnetic resonance and elemental analyses. The antioxidant activity of 4-aminoantipyrine and prepared complexes were studied by two different methods; Free radical scavenging activity DPPH and CUPRRAC methods. Tri and di-tin complexes gave high percentage inhibition than ligand with both methods due to tin moiety, also triphenyltin carboxylate complex was the best compared with the others. \u0000 \u0000KEY WORDS: 4-Aminoantipyrine, Condensation, Triphenyl tin chloride, DPPH and CUPRRAC methods \u0000Bull. Chem. Soc. Ethiop. 2023, 37(5), 1163-1170. \u0000DOI: https://dx.doi.org/10.4314/bcse.v37i5.9","PeriodicalId":9501,"journal":{"name":"Bulletin of the Chemical Society of Ethiopia","volume":" ","pages":""},"PeriodicalIF":1.2,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"48731232","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Umang A. Gosalia, Manish Srivastava, Neetu Yaduvanshi, Shivangi Jaiswal, Sonika Jain, D. Kishore, J. Dwivedi, Swapnil Sharma
ABSTRACT. Novel five-membered ring (pyrrole, pyrazole and imidazole)-based pyrimidine and quinazoline derivatives were synthesized by one-pot domino approach. This approach has the advantages of high yield, mild reaction conditions and a simple work-up procedure. The structure of the synthesized compound was elucidated by spectroscopy technique and elemental analysis. The synthesized compound were examined for antimicrobial activity against four bacteria (E. coli, S. pyogenes, S. aureus, and P. aeruginosa) and two fungi (C. albicans and A. clavatus) and most of the synthesized compound exhibited moderate to good activity against reference drug ampicillin, ciprofloxacin, norfloxacin, gentamycin, nystatin and griseofulvin, respectively. KEY WORDS: One-pot, Pyrrole, Pyrazole, Imidazole, Pyrimidine, Quinazoline, Antimicrobial activity Bull. Chem. Soc. Ethiop. 2023, 37(5), 1193-1208. DOI: https://dx.doi.org/10.4314/bcse.v37i5.12
{"title":"One-pot mediated synthesis of pyrimidine and quinazoline annulated derivatives of nitrogen containing five membered rings through their nitrile derivatives as antibacterial agents","authors":"Umang A. Gosalia, Manish Srivastava, Neetu Yaduvanshi, Shivangi Jaiswal, Sonika Jain, D. Kishore, J. Dwivedi, Swapnil Sharma","doi":"10.4314/bcse.v37i5.12","DOIUrl":"https://doi.org/10.4314/bcse.v37i5.12","url":null,"abstract":"ABSTRACT. Novel five-membered ring (pyrrole, pyrazole and imidazole)-based pyrimidine and quinazoline derivatives were synthesized by one-pot domino approach. This approach has the advantages of high yield, mild reaction conditions and a simple work-up procedure. The structure of the synthesized compound was elucidated by spectroscopy technique and elemental analysis. The synthesized compound were examined for antimicrobial activity against four bacteria (E. coli, S. pyogenes, S. aureus, and P. aeruginosa) and two fungi (C. albicans and A. clavatus) and most of the synthesized compound exhibited moderate to good activity against reference drug ampicillin, ciprofloxacin, norfloxacin, gentamycin, nystatin and griseofulvin, respectively. \u0000 \u0000KEY WORDS: One-pot, Pyrrole, Pyrazole, Imidazole, Pyrimidine, Quinazoline, Antimicrobial activity \u0000 \u0000Bull. Chem. Soc. Ethiop. 2023, 37(5), 1193-1208. \u0000DOI: https://dx.doi.org/10.4314/bcse.v37i5.12","PeriodicalId":9501,"journal":{"name":"Bulletin of the Chemical Society of Ethiopia","volume":" ","pages":""},"PeriodicalIF":1.2,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45195214","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Amnah Mohammed Alsuhaibani, Abdel Majid A. Adam, M. S. Refat, Mohamed I. Kobeasy, S. B. Bakare, Eman Salah Bushara
ABSTRACT. The condensation of thiosemicarbazide with oxazolidinone produced 5-benzylidene-3-(4-chloro-phenyl)-6-oxo-5,6-dihydro-1H-[1,2,4]triazine-2-carbothioic acid amide (HL1). Co(II) and Ni(II) ions were reacted with the HL1 ligand. Elemental analysis and molar conductivity, along with mass, 1H-NMR, IR, UV-Vis, and X-ray powder diffraction spectral examinations, were used to reveal the chemical structure of the synthesized complexes. The stoichiometry of the complexes was determined to be 1:2 (metallic: moiety) using analytical, spectroscopic, and thermal data. The thermal properties of the complexes were explored using thermogravimetric (TG-DTG/DTA) methods, as well as the decomposition stages. Several kinetic thermodynamic parameters such as free activation energy (ΔG*), activation enthalpy (ΔH*), activation entropy (ΔS*), pre-exponential factor (A), and the activation energy (E*) were estimated. Inhibitory effects towards colon carcinoma cells (HCT cell line), hepatocellular carcinoma (Hep G2 cell line), and breast carcinoma (MCF-7 cell line) were verified using various concentrations of the samples. A colorimetric method was used to determine the cell viability percent in comparison to doxorubicin drug as a control. KEY WORDS: 1,2,4-Triazines, Thiosemicarbazide, Thermogravimetric analysis, Non-electrolytes, Anticancer Bull. Chem. Soc. Ethiop. 2023, 37(5), 1151-1162. DOI: https://dx.doi.org/10.4314/bcse.v37i5.8
{"title":"Spectroscopic, thermal, and anticancer investigations of new cobalt(II) and nickel(II) triazine complexes","authors":"Amnah Mohammed Alsuhaibani, Abdel Majid A. Adam, M. S. Refat, Mohamed I. Kobeasy, S. B. Bakare, Eman Salah Bushara","doi":"10.4314/bcse.v37i5.8","DOIUrl":"https://doi.org/10.4314/bcse.v37i5.8","url":null,"abstract":"ABSTRACT. The condensation of thiosemicarbazide with oxazolidinone produced 5-benzylidene-3-(4-chloro-phenyl)-6-oxo-5,6-dihydro-1H-[1,2,4]triazine-2-carbothioic acid amide (HL1). Co(II) and Ni(II) ions were reacted with the HL1 ligand. Elemental analysis and molar conductivity, along with mass, 1H-NMR, IR, UV-Vis, and X-ray powder diffraction spectral examinations, were used to reveal the chemical structure of the synthesized complexes. The stoichiometry of the complexes was determined to be 1:2 (metallic: moiety) using analytical, spectroscopic, and thermal data. The thermal properties of the complexes were explored using thermogravimetric (TG-DTG/DTA) methods, as well as the decomposition stages. Several kinetic thermodynamic parameters such as free activation energy (ΔG*), activation enthalpy (ΔH*), activation entropy (ΔS*), pre-exponential factor (A), and the activation energy (E*) were estimated. Inhibitory effects towards colon carcinoma cells (HCT cell line), hepatocellular carcinoma (Hep G2 cell line), and breast carcinoma (MCF-7 cell line) were verified using various concentrations of the samples. A colorimetric method was used to determine the cell viability percent in comparison to doxorubicin drug as a control. \u0000 \u0000KEY WORDS: 1,2,4-Triazines, Thiosemicarbazide, Thermogravimetric analysis, Non-electrolytes, Anticancer \u0000Bull. Chem. Soc. Ethiop. 2023, 37(5), 1151-1162. \u0000DOI: https://dx.doi.org/10.4314/bcse.v37i5.8","PeriodicalId":9501,"journal":{"name":"Bulletin of the Chemical Society of Ethiopia","volume":" ","pages":""},"PeriodicalIF":1.2,"publicationDate":"2023-06-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47218999","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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