Pub Date : 2020-03-03DOI: 10.26655/jmchemsci.2020.3.3
D. Nartop, H. Öğütcü
In this research study, three new unsymmetric diimines (3a-3c) were prepared using a two-step process. The synthesized unsymmetric tetradentate diimines were elucidated by FT-IR, 1H-NMR, LC-MS, elemental analysis techniques. The antimicrobial and the antifungal properties of newly synthesized unsymmetrical diimines (3a-3c) and previously reported by one of us unsymmetrical diimines (4a-4c) were evaluated against L. monocytogenes 4b, B. cereus sp., S. typhi H, Br. abortus, S. epidermis sp., M. Luteus sp., E. coli, P. putida sp. Sh. dys. typ. 7 ve C. albicans. 3b, 3c, 4a and 4c are showed the highest antimicrobial activity against B.cereus sp. 3a and 4b are exhibited the highest activity against S.epidermis sp. and Br. abortus, respectively. In addition, all unsymmetrical diimines are showed high antifungal activity against C. albicans.
本研究采用两步法合成了三种新的不对称二亚胺(3a-3c)。通过FT-IR、1H-NMR、LC-MS、元素分析等手段对合成的非对称四齿二亚胺进行了表征。对新合成的不对称二亚胺(3a-3c)和已有报道的不对称二亚胺(4a-4c)对单核增生L. L. 4b、蜡样芽孢杆菌、斑疹伤寒S. H、Br。流产杆菌、表皮葡萄球菌、黄体芽孢杆菌、大肠杆菌、恶臭杆菌等。typ。7 .白色念珠菌。其中3b、3c、4a和4c对蜡样芽孢杆菌的抑菌活性最高，3a和4b对表皮芽孢杆菌和Br的抑菌活性最高。分别流产。此外，所有非对称二亚胺对白色念珠菌均表现出较高的抗真菌活性。
{"title":"Novel unsymmetric diimines: Synthesis and biological evaluation against pathogenic microorganisms","authors":"D. Nartop, H. Öğütcü","doi":"10.26655/jmchemsci.2020.3.3","DOIUrl":"https://doi.org/10.26655/jmchemsci.2020.3.3","url":null,"abstract":"In this research study, three new unsymmetric diimines (3a-3c) were prepared using a two-step process. The synthesized unsymmetric tetradentate diimines were elucidated by FT-IR, 1H-NMR, LC-MS, elemental analysis techniques. The antimicrobial and the antifungal properties of newly synthesized unsymmetrical diimines (3a-3c) and previously reported by one of us unsymmetrical diimines (4a-4c) were evaluated against L. monocytogenes 4b, B. cereus sp., S. typhi H, Br. abortus, S. epidermis sp., M. Luteus sp., E. coli, P. putida sp. Sh. dys. typ. 7 ve C. albicans. 3b, 3c, 4a and 4c are showed the highest antimicrobial activity against B.cereus sp. 3a and 4b are exhibited the highest activity against S.epidermis sp. and Br. abortus, respectively. In addition, all unsymmetrical diimines are showed high antifungal activity against C. albicans.","PeriodicalId":16365,"journal":{"name":"Journal of Medicinal and Chemical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2020-03-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73041377","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-01DOI: 10.26655/JMCHEMSCI.2019.8.1
Fardous Bobtana, Fakhri A. Elabbar, N. Bader
The potential of Hammada scoparia (Hamm.) and Halocnemum Strobilaceum (Halo.) growing in Benghazi-Libya for soil phytoremediation purpose has been evaluated. Hammada scoparia (Hamm.) and Halocnemum Strobilaceum (Halo.) and their roots soil samples were collected and analyzed for Cd, Ni and Pb concentrations in a salty area in the north coastal region of Benghazi, near Benghazi asphalt factory, Benghazi steel factory, Brega oil company sorage tanks, and north Benghazi power station. The biological absorption coefficient (BAC), bioconcentration factor (BCF), and translocation factor (TF) of Hammada scoparia and Halocnemum Strobilaceum have been calculated. Both plants are moderate extractor, they tend to phytoextraction process except Halo tends strongly to phytostabiliztion process in case of Cu and Fe.
{"title":"Evaluation of Halocnemum strobilaceum and Hammada scoparia plants performance for contaminated soil phytoremediation","authors":"Fardous Bobtana, Fakhri A. Elabbar, N. Bader","doi":"10.26655/JMCHEMSCI.2019.8.1","DOIUrl":"https://doi.org/10.26655/JMCHEMSCI.2019.8.1","url":null,"abstract":"The potential of Hammada scoparia (Hamm.) and Halocnemum Strobilaceum (Halo.) growing in Benghazi-Libya for soil phytoremediation purpose has been evaluated. Hammada scoparia (Hamm.) and Halocnemum Strobilaceum (Halo.) and their roots soil samples were collected and analyzed for Cd, Ni and Pb concentrations in a salty area in the north coastal region of Benghazi, near Benghazi asphalt factory, Benghazi steel factory, Brega oil company sorage tanks, and north Benghazi power station. The biological absorption coefficient (BAC), bioconcentration factor (BCF), and translocation factor (TF) of Hammada scoparia and Halocnemum Strobilaceum have been calculated. Both plants are moderate extractor, they tend to phytoextraction process except Halo tends strongly to phytostabiliztion process in case of Cu and Fe.","PeriodicalId":16365,"journal":{"name":"Journal of Medicinal and Chemical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78534968","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-01DOI: 10.26655/JMCHEMSCI.2019.8.3
H. Nasiri, B. Ceylan, Katharina F. Hohmann, M. Kaiser, H. Schwalbe
A set of conformationally restricted analogues of the natural product primin were synthesized as potential antiprotozoal agents. The synthesis utilizes quinone C-H functionalization methods to enable an efficient and easy access to primin analogues. The antiprotozoal activities of this series were evaluated in a panel of parasites and compared with the natural product primin. For all synthesized primin analogues a potent in vitro activity was found against the pathogen Trypanosoma brucei rhodesiense (IC50 < 0.05 µg/mL). The observed antiprotozoal activity is not related to production of reactive oxygen species (ROS). Initial results of the in vivo experiments with a T. b. rhodesiense rodent animal model of the human disease were also reported. Intraperitoneal injection administration of compound 7 resulted in complete clearance of T. b. rhodesiense in tested rodent animals 24 hours after the last treatment. Our results show that the primin scaffold represents a new scaffold for further development of potent inhibitors of Trypanosoma brucei rhodesiense.
{"title":"Design, Synthesis, and Testing of Antiprotozoal Activity of Primin and Analogues","authors":"H. Nasiri, B. Ceylan, Katharina F. Hohmann, M. Kaiser, H. Schwalbe","doi":"10.26655/JMCHEMSCI.2019.8.3","DOIUrl":"https://doi.org/10.26655/JMCHEMSCI.2019.8.3","url":null,"abstract":"A set of conformationally restricted analogues of the natural product primin were synthesized as potential antiprotozoal agents. The synthesis utilizes quinone C-H functionalization methods to enable an efficient and easy access to primin analogues. The antiprotozoal activities of this series were evaluated in a panel of parasites and compared with the natural product primin. For all synthesized primin analogues a potent in vitro activity was found against the pathogen Trypanosoma brucei rhodesiense (IC50 < 0.05 µg/mL). The observed antiprotozoal activity is not related to production of reactive oxygen species (ROS). Initial results of the in vivo experiments with a T. b. rhodesiense rodent animal model of the human disease were also reported. Intraperitoneal injection administration of compound 7 resulted in complete clearance of T. b. rhodesiense in tested rodent animals 24 hours after the last treatment. Our results show that the primin scaffold represents a new scaffold for further development of potent inhibitors of Trypanosoma brucei rhodesiense.","PeriodicalId":16365,"journal":{"name":"Journal of Medicinal and Chemical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89941544","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-01DOI: 10.26655/JMCHEMSCI.2019.8.5
Attah S. Izuchi, Efeturi A. Onoabedje, O. Ekoh, S. Okafor, U. Okoro
Synthesis of new medicinally important phenylsulphonyl aminoalkanamides and N-aryl p-toluene sulphonamides is reported. The reaction between benzenesulphonylchloride 7 with valine gave 3-methyl-2-[phenylsulphonyl)amino]butanoic acid 9 which is converted into 2-[acetyl (phenylsulphonyl) amino]-3-methyl butanoic acid 10 by reaction with acetic anhydride in acetic acid. The reaction of the later with SOCl2 and subsequently with NH3 afforded 2-[N-acetyl (phenylsulphonyl) amino]-3-methyl butanamide intermediate 11. The palladium catalysed reaction of the intermediate with readily available aryl chlorides and bromides afforded a variety of phenyl sulphonylaminoalkanamides 13a-c. In another synthesis, p-toluenesulphonylchloride (14) reacted with aqueous ammonia to give 4-methyl benzenesulphonamide 15 which is converted into N-(4-hydroxylphenyl)-4-methylbenzene sulphonamide 17a, N-(4-formyl phenyl)-4-methyl benzene sulphonamide 17b, N-(4-aminophenyl)-4-methyl benzenesulphonamide 17c, 4-methyl-N-(2-methylphenyl) benzene sulphonamide 17d, N-(4-Methoxyphenyl)-4-methyl benzenesulphonamide 17e in good yields, by reaction with 4-chlorophenol, 4-bromobenzaldehyde , 4-bromoaniline, 2-chlorotoluene and 1-bromo-2-methoxybenzene, respectively. Structures of the synthesized compounds were confirmed by spectroscopic and elemental analytical data
{"title":"Synthesis of Medicinally Relevant Phenyl Sulphonylamino Alkanamides and N-aryl P-toluenesulphonamides","authors":"Attah S. Izuchi, Efeturi A. Onoabedje, O. Ekoh, S. Okafor, U. Okoro","doi":"10.26655/JMCHEMSCI.2019.8.5","DOIUrl":"https://doi.org/10.26655/JMCHEMSCI.2019.8.5","url":null,"abstract":"Synthesis of new medicinally important phenylsulphonyl aminoalkanamides and N-aryl p-toluene sulphonamides is reported. The reaction between benzenesulphonylchloride 7 with valine gave 3-methyl-2-[phenylsulphonyl)amino]butanoic acid 9 which is converted into 2-[acetyl (phenylsulphonyl) amino]-3-methyl butanoic acid 10 by reaction with acetic anhydride in acetic acid. The reaction of the later with SOCl2 and subsequently with NH3 afforded 2-[N-acetyl (phenylsulphonyl) amino]-3-methyl butanamide intermediate 11. The palladium catalysed reaction of the intermediate with readily available aryl chlorides and bromides afforded a variety of phenyl sulphonylaminoalkanamides 13a-c. In another synthesis, p-toluenesulphonylchloride (14) reacted with aqueous ammonia to give 4-methyl benzenesulphonamide 15 which is converted into N-(4-hydroxylphenyl)-4-methylbenzene sulphonamide 17a, N-(4-formyl phenyl)-4-methyl benzene sulphonamide 17b, N-(4-aminophenyl)-4-methyl benzenesulphonamide 17c, 4-methyl-N-(2-methylphenyl) benzene sulphonamide 17d, N-(4-Methoxyphenyl)-4-methyl benzenesulphonamide 17e in good yields, by reaction with 4-chlorophenol, 4-bromobenzaldehyde , 4-bromoaniline, 2-chlorotoluene and 1-bromo-2-methoxybenzene, respectively. Structures of the synthesized compounds were confirmed by spectroscopic and elemental analytical data","PeriodicalId":16365,"journal":{"name":"Journal of Medicinal and Chemical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72842825","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-01DOI: 10.26655/JMCHEMSCI.2019.8.8
Ebtihal Almadani Alforjany, Ruwida Kamour
This study is carried out to test the stability of antibiotic dry suspensions reconstituted with various water temperatures. The testing included physical, microbial and chemical changes of samples reconstituted with water at 40, 60, 70 and 80ᵒC. These changes were compared to control samples prepared with water at temperature 25ᵒC. HPLC method was followed qualitatively to identify antibiotic active constituent in addition to quantitative analysis to evaluate antibiotic contents compared to control samples. The changes were assessed within one hour after reconstitution and after four days of reconstitution. Physical tests showed changes of amoxicillinclavulenic acid suspension’s colour prepared at 80ᵒC. Sedimentation ratio, sedimentation rate and sedimentation volume decreased as temperature increased were these parameters were tested only for amoxicillin suspension. Upon centrifugation there was a decrease in sediment volume accompanied with an increase in supernatant volume resulting in changes in sediment/supernatant ratio. Microbial study showed a marked decrease in antimicrobial activity for both amoxicillin and amoxicillin/clavulenic acid suspensions. HPLC results showed a decrease in amoxicillin and clavulanate in samples prepared with heated water compared to those prepared with cooled water at 25ᵒC.
{"title":"Effect of Temperature of Water Used For Reconstitution On Stability Of Antibiotic Dry Suspension","authors":"Ebtihal Almadani Alforjany, Ruwida Kamour","doi":"10.26655/JMCHEMSCI.2019.8.8","DOIUrl":"https://doi.org/10.26655/JMCHEMSCI.2019.8.8","url":null,"abstract":"This study is carried out to test the stability of antibiotic dry suspensions reconstituted with various water temperatures. The testing included physical, microbial and chemical changes of samples reconstituted with water at 40, 60, 70 and 80ᵒC. These changes were compared to control samples prepared with water at temperature 25ᵒC. HPLC method was followed qualitatively to identify antibiotic active constituent in addition to quantitative analysis to evaluate antibiotic contents compared to control samples. The changes were assessed within one hour after reconstitution and after four days of reconstitution. Physical tests showed changes of amoxicillinclavulenic acid suspension’s colour prepared at 80ᵒC. Sedimentation ratio, sedimentation rate and sedimentation volume decreased as temperature increased were these parameters were tested only for amoxicillin suspension. Upon centrifugation there was a decrease in sediment volume accompanied with an increase in supernatant volume resulting in changes in sediment/supernatant ratio. Microbial study showed a marked decrease in antimicrobial activity for both amoxicillin and amoxicillin/clavulenic acid suspensions. HPLC results showed a decrease in amoxicillin and clavulanate in samples prepared with heated water compared to those prepared with cooled water at 25ᵒC.","PeriodicalId":16365,"journal":{"name":"Journal of Medicinal and Chemical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74756701","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-01DOI: 10.26655/JMCHEMSCI.2019.8.2
H. Louis, Hamzart Adejoke, O. Amusan
The importance of natural products in the pharmaceutical industry cannot be abated because it plays a vital role in the prevention and treatments of diseases such as cancer, malaria, pile etc. These natural products e.g. alkaloid, flavonoid, phenol, saponin, and tannin are bioactive compounds in a plant which are essential in plant metabolic activities. All of these including alkaloids has been tested for their huge medicinal properties hence, serves as an alternative medicine. Although, through the modern-day technologies, these bioactive compounds are separated from the plants and synthesized into capsules and tablets for easy administration, usage, and storage. The manner of poisoning with plants can be due to unintentional ingestion, affordability, and availability, excess ingestion, improper methods of extraction and purification of plant materials. In some cases, the resultant effect(s) of these poisoning may cause serious illness, injury or even death. Thus, this review gives an overview of the pharmacological importance of named alkaloids, toxicology and methods of extraction and purification of alkaloids in the plant. Furthermore, this review will provide information to researchers to further investigate the medicinal potentials of these alkaloids, help in the development of new drugs for the treatment of various diseases, creates awareness on the side-effects of excess or abuse of medicinal plants and finally encourages rational use of natural resources for sustainability.
{"title":"A Review on Classes, Extraction, Purification and Pharmaceutical Importance of Plants Alkaloid","authors":"H. Louis, Hamzart Adejoke, O. Amusan","doi":"10.26655/JMCHEMSCI.2019.8.2","DOIUrl":"https://doi.org/10.26655/JMCHEMSCI.2019.8.2","url":null,"abstract":"The importance of natural products in the pharmaceutical industry cannot be abated because it plays a vital role in the prevention and treatments of diseases such as cancer, malaria, pile etc. These natural products e.g. alkaloid, flavonoid, phenol, saponin, and tannin are bioactive compounds in a plant which are essential in plant metabolic activities. All of these including alkaloids has been tested for their huge medicinal properties hence, serves as an alternative medicine. Although, through the modern-day technologies, these bioactive compounds are separated from the plants and synthesized into capsules and tablets for easy administration, usage, and storage. The manner of poisoning with plants can be due to unintentional ingestion, affordability, and availability, excess ingestion, improper methods of extraction and purification of plant materials. In some cases, the resultant effect(s) of these poisoning may cause serious illness, injury or even death. Thus, this review gives an overview of the pharmacological importance of named alkaloids, toxicology and methods of extraction and purification of alkaloids in the plant. Furthermore, this review will provide information to researchers to further investigate the medicinal potentials of these alkaloids, help in the development of new drugs for the treatment of various diseases, creates awareness on the side-effects of excess or abuse of medicinal plants and finally encourages rational use of natural resources for sustainability.","PeriodicalId":16365,"journal":{"name":"Journal of Medicinal and Chemical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86904755","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-07-01DOI: 10.26655/JMCHEMSCI.2019.8.4
A. Usman, V. Thoss, M. Nur-E-Alam
A new compound, catechin-3-O-α-L-rhamnopyranosyl (1→4) β-D-glucopyranoside was isolated from the ethylacetate soluble fraction of the aqueous extract of the whole seeds of Trichilia emetica (Family: Meliaceae). The structure of this compound was established on the basis of nuclear magnetic resonance (NMR), Infrared (IR) spectroscopy and ultraviolet-visible (UV-vis) spectrophotometry. The compound was also subjected to antimicrobial activity and brine shrimp lethality bioassay. The pure compound showed either no or reduced activity against microorganisms tested, it also showed no cytotoxicity.
从吐毛毛菌(Trichilia emetica)全种子水提物的乙酸乙酯可溶性部分中分离得到一个新的化合物儿茶素-3- o -α-L-rhamnopyranosyl(1→4)β- d -葡萄糖吡喃苷。通过核磁共振(NMR)、红外(IR)和紫外-可见(UV-vis)分光光度法确定了该化合物的结构。并对该化合物进行了抗菌活性和盐水对虾致死性生物测定。纯化合物对微生物没有活性或活性降低，也没有细胞毒性。
{"title":"A new flavonoid glycoside from Trichilia emetica","authors":"A. Usman, V. Thoss, M. Nur-E-Alam","doi":"10.26655/JMCHEMSCI.2019.8.4","DOIUrl":"https://doi.org/10.26655/JMCHEMSCI.2019.8.4","url":null,"abstract":"A new compound, catechin-3-O-α-L-rhamnopyranosyl (1→4) β-D-glucopyranoside was isolated from the ethylacetate soluble fraction of the aqueous extract of the whole seeds of Trichilia emetica (Family: Meliaceae). The structure of this compound was established on the basis of nuclear magnetic resonance (NMR), Infrared (IR) spectroscopy and ultraviolet-visible (UV-vis) spectrophotometry. The compound was also subjected to antimicrobial activity and brine shrimp lethality bioassay. The pure compound showed either no or reduced activity against microorganisms tested, it also showed no cytotoxicity.","PeriodicalId":16365,"journal":{"name":"Journal of Medicinal and Chemical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-07-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"73510875","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-05-01DOI: 10.26655/JMCHEMSCI.2019.4.6
N. Manju, B. Kalluraya, Asma, S. Madankumar, B. C. Revanasiddappa, Chandra
In this paper, we describe a simplecatalyst-free protocol for the synthesis of thiazole, thiazolone integrated pyrazole derivatives, under ultra-sonication technique. Thiazolone derivatives 5a, 5e, 5i, 5d, 5h, 5l were derived from [2+3] cyclocondensation reaction between carbothioamide pyrazoline (4 a-c) as S-N bi-nucleophile with DMAD/DEAD. The target molecules 5b, 5f, 5j,5c, 5g, 5k weresynthesized by reaction of (4 a-c) with substituted bromoethanone. Formation of the products was confirmed by FT-IR, 1H-NMR, 13C-NMR, LC-MS and X-ray analysis. Docking studies were carried out against the antimicrobial target (3UDI) to know interaction of the molecules (ligands) with the docked target. Among the docked compounds thiazolone derivative 5d showed the minimum binding energy of -9.08 kJ/mol with ligand efficiency of -0.23. All the synthesized compounds were examined primarily for their in-vitro antibacterial and antioxidant activity (IC50). Compound 5g (18±0.0) and 5d (19.5±0.5) showed significant bacterial inhibition against E.coli and S.aureus. Compound 5k (16.57) were showed substantial DPPH free radical inhibition activity as compared to the reference drug Ascorbic acid.
{"title":"Ultrasound-assisted synthesis of auxiliary pyrazoline integrated thiazole, thiazolone derivative and their biological evaluation","authors":"N. Manju, B. Kalluraya, Asma, S. Madankumar, B. C. Revanasiddappa, Chandra","doi":"10.26655/JMCHEMSCI.2019.4.6","DOIUrl":"https://doi.org/10.26655/JMCHEMSCI.2019.4.6","url":null,"abstract":"In this paper, we describe a simplecatalyst-free protocol for the synthesis of thiazole, thiazolone integrated pyrazole derivatives, under ultra-sonication technique. Thiazolone derivatives 5a, 5e, 5i, 5d, 5h, 5l were derived from [2+3] cyclocondensation reaction between carbothioamide pyrazoline (4 a-c) as S-N bi-nucleophile with DMAD/DEAD. The target molecules 5b, 5f, 5j,5c, 5g, 5k weresynthesized by reaction of (4 a-c) with substituted bromoethanone. Formation of the products was confirmed by FT-IR, 1H-NMR, 13C-NMR, LC-MS and X-ray analysis. Docking studies were carried out against the antimicrobial target (3UDI) to know interaction of the molecules (ligands) with the docked target. Among the docked compounds thiazolone derivative 5d showed the minimum binding energy of -9.08 kJ/mol with ligand efficiency of -0.23. All the synthesized compounds were examined primarily for their in-vitro antibacterial and antioxidant activity (IC50). Compound 5g (18±0.0) and 5d (19.5±0.5) showed significant bacterial inhibition against E.coli and S.aureus. Compound 5k (16.57) were showed substantial DPPH free radical inhibition activity as compared to the reference drug Ascorbic acid.","PeriodicalId":16365,"journal":{"name":"Journal of Medicinal and Chemical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81561420","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-05-01DOI: 10.26655/JMCHEMSCI.2019.4.7
R. Kaur, Kapil Kumar
An efficient procedure was developed for the synthesis of different derivatives of 3,4-disubstituted pyrrole using TosMIC with ethyl cinnamate in DMF using lithium hydroxide monohydrate as a base. Further, trisubstituted pyrrole was synthesized using nitrostyrene, ethyl-propiolate and benzylamine in toluene as a reaction medium. This reaction was catalysed by lewis acid FeCl3. This strategy was further modified to synthesized tetra and penta substituted pyrrole using ethanol as a reaction medium keeping other conditions intact. This method is very economical and was successfully utilized for the synthesis of its derivatives with moderate to good yields.
{"title":"A Journey Towards FeCl3 Catalysed Synthesis of Multisubstituted Pyrrole","authors":"R. Kaur, Kapil Kumar","doi":"10.26655/JMCHEMSCI.2019.4.7","DOIUrl":"https://doi.org/10.26655/JMCHEMSCI.2019.4.7","url":null,"abstract":"An efficient procedure was developed for the synthesis of different derivatives of 3,4-disubstituted pyrrole using TosMIC with ethyl cinnamate in DMF using lithium hydroxide monohydrate as a base. Further, trisubstituted pyrrole was synthesized using nitrostyrene, ethyl-propiolate and benzylamine in toluene as a reaction medium. This reaction was catalysed by lewis acid FeCl3. This strategy was further modified to synthesized tetra and penta substituted pyrrole using ethanol as a reaction medium keeping other conditions intact. This method is very economical and was successfully utilized for the synthesis of its derivatives with moderate to good yields.","PeriodicalId":16365,"journal":{"name":"Journal of Medicinal and Chemical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84406102","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-05-01DOI: 10.26655/JMCHEMSCI.2019.4.5
Sadiq Abdurrahman Abubakar Shawai, Muhammad Sani Nahannu, H. Mukhtar, I. M. Isma'il
Human activities are a major factor determining the quality of surface and groundwater through atmospheric pollution, effluent discharges, use of agricultural chemicals, eroded soil and land use.The purpose of this research was to determine the physicochemical parameters of water samples collected from Sa’adatu Rimi College of Education, Kumbotso Kano and to compare with the standards given by World Health Organization (WHO) and Nigeria Standard for Drinking Water Quality (NSDWQ). Four samples were collected from different locations within the college premises for the analysis. The analyzed parameters are pH, temperature, Total dissolved solids, Total suspended solids, Suspended solid, Electrical conductivity, Alkalinity, Mg2+,Ca2+, ammonia, sulphate,Nitrate, Nitrite,Turbidity, Salinity, Total hardness, free carbon dioxide, Iron and Chloride. The results indicated that all the analyzed parameters are within the permissible limits recommended byWHO and NSDWQwith exception of turbidity level at A sampling station, pH concentration at B, C, and D sampling point and nitriteconcentrations at C and D sampling point. The results also showed that, the concentration of total hardness were slightly above the maximum permissible limit (MPL) recommended by NSDWQ. This paper also recommended that, the college management should provide a basis for the regular monitoring of water quality status.
人类活动是通过大气污染、废水排放、农用化学品的使用、土壤侵蚀和土地利用来决定地表水和地下水质量的一个主要因素。这项研究的目的是确定从Kumbotso Kano Sa 'adatu Rimi教育学院收集的水样的物理化学参数，并与世界卫生组织(世卫组织)和尼日利亚饮用水质量标准(NSDWQ)给出的标准进行比较。四个样本从学院内的不同地点收集进行分析。分析的参数有pH、温度、总溶解固体、总悬浮固体、悬浮固体、电导率、碱度、Mg2+、Ca2+、氨、硫酸盐、硝酸盐、亚硝酸盐、浊度、盐度、总硬度、游离二氧化碳、铁和氯化物。结果表明，除A采样点浊度、B、C、D采样点pH浓度和C、D采样点亚硝酸盐浓度外，分析参数均在who和nsdwq推荐的允许范围内。结果还表明，总硬度浓度略高于NSDWQ推荐的最大允许限值(MPL)。本文还建议，为高校管理部门定期监测水质状况提供依据。
{"title":"ASSESMENT OF GROUNDWATER SAMPLES FROM SA'ADATU RIMI COLLEGE OF EDUCATION, KUMBOTSO, KANO","authors":"Sadiq Abdurrahman Abubakar Shawai, Muhammad Sani Nahannu, H. Mukhtar, I. M. Isma'il","doi":"10.26655/JMCHEMSCI.2019.4.5","DOIUrl":"https://doi.org/10.26655/JMCHEMSCI.2019.4.5","url":null,"abstract":"Human activities are a major factor determining the quality of surface and groundwater through atmospheric pollution, effluent discharges, use of agricultural chemicals, eroded soil and land use.The purpose of this research was to determine the physicochemical parameters of water samples collected from Sa’adatu Rimi College of Education, Kumbotso Kano and to compare with the standards given by World Health Organization (WHO) and Nigeria Standard for Drinking Water Quality (NSDWQ). Four samples were collected from different locations within the college premises for the analysis. The analyzed parameters are pH, temperature, Total dissolved solids, Total suspended solids, Suspended solid, Electrical conductivity, Alkalinity, Mg2+,Ca2+, ammonia, sulphate,Nitrate, Nitrite,Turbidity, Salinity, Total hardness, free carbon dioxide, Iron and Chloride. The results indicated that all the analyzed parameters are within the permissible limits recommended byWHO and NSDWQwith exception of turbidity level at A sampling station, pH concentration at B, C, and D sampling point and nitriteconcentrations at C and D sampling point. The results also showed that, the concentration of total hardness were slightly above the maximum permissible limit (MPL) recommended by NSDWQ. This paper also recommended that, the college management should provide a basis for the regular monitoring of water quality status.","PeriodicalId":16365,"journal":{"name":"Journal of Medicinal and Chemical Sciences","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2019-05-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77453610","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：