Pub Date : 2022-01-01DOI: 10.5267/j.ccl.2022.4.004
M. F. Dhaduk, H. Joshi
A series of isoxazole derivatives, 3-aryl-5-[5-(4-nitrophenyl)-2-furyl]-2,3-dihydroisoxazoles (5a-j) were synthesized by cyclocondensation reaction between 1-aryl-3-[5-(4-nitrophenyl)-2-furyl]prop-2-en-1-ones (4a-j) and hydroxylamine hydrochloride in presence of sodium acetate in glacial acetic acid at reflux temperature. Formerly, compounds (4a-j) were synthesized by the condensation of 5-(4-nitrophenyl) furan-2-carbaldehyde (3) with various aromatic ketones by using alkali as catalyst. The structures of the synthesized various isoxazole have been characterized by using elemental analysis, Infrared,1H-NMR spectroscopy and further supported by Mass spectroscopy. All the products have been screened for their in-vitro biological assay like antibacterial activity towards Gram-positive and Gram-negative bacterial strains and antifungal activity towards Aspergillus niger at a concentration of 40 µg/ml. It was exposed that the compounds 5a, 5c, 5e, 5f, and 5i showed inspiring antibacterial and antifungal activity compared to the used reference standard.
{"title":"Synthesis, characterization and antimicrobial activity of some new isoxazole derivatives","authors":"M. F. Dhaduk, H. Joshi","doi":"10.5267/j.ccl.2022.4.004","DOIUrl":"https://doi.org/10.5267/j.ccl.2022.4.004","url":null,"abstract":"A series of isoxazole derivatives, 3-aryl-5-[5-(4-nitrophenyl)-2-furyl]-2,3-dihydroisoxazoles (5a-j) were synthesized by cyclocondensation reaction between 1-aryl-3-[5-(4-nitrophenyl)-2-furyl]prop-2-en-1-ones (4a-j) and hydroxylamine hydrochloride in presence of sodium acetate in glacial acetic acid at reflux temperature. Formerly, compounds (4a-j) were synthesized by the condensation of 5-(4-nitrophenyl) furan-2-carbaldehyde (3) with various aromatic ketones by using alkali as catalyst. The structures of the synthesized various isoxazole have been characterized by using elemental analysis, Infrared,1H-NMR spectroscopy and further supported by Mass spectroscopy. All the products have been screened for their in-vitro biological assay like antibacterial activity towards Gram-positive and Gram-negative bacterial strains and antifungal activity towards Aspergillus niger at a concentration of 40 µg/ml. It was exposed that the compounds 5a, 5c, 5e, 5f, and 5i showed inspiring antibacterial and antifungal activity compared to the used reference standard.","PeriodicalId":10942,"journal":{"name":"Current Chemistry Letters","volume":"41 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81534848","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 : 2022-01-01DOI: 10.5267/j.ccl.2021.10.001
S. A. Abdel-Raheem, A. El-Dean, M. A. A. ul-Malik, R. Hassanien, M. El-sayed, Aly A. Abd-Ella, Sameh A. Zawam, M. Tolba
In examining for unique insecticidal agents, two derivatives namely, 2-((3-cyano-4,6-distyrylpyridin-2-yl)thio)-N-(4-nitrophenyl)acetamide (2) and 3-amino-N-(4-nitrophenyl)-4,6-distyrylthieno[2,3-b]pyridine-2-carboxamide (3) were synthesized from distyrylpyridine-2-thione (1). The new compounds were structurally clarified by spectral and elemental analysis data. The insecticidal activity of these compounds were carried out against cowpea aphid, Aphis craccivora Koch. It is demonstrated that the compounds 2 and 3 have noteworthy insecticidal activity against nymphs of cowpea aphid with LC50 values of 0.025-0.027 ppm and 0.005-0.006 ppm after 24 h and 48 h of treatment, respectively. Also, the compounds 2 and 3 have noteworthy insecticidal activity against adults of cowpea aphid with LC50 values of 0.112-0.129 ppm and 0.014-0.015 ppm after 24 h and 48 h of treatment, respectively, that were comparable to that of the control acetamiprid.
{"title":"Synthesis of new distyrylpyridine analogues bearing amide substructure as effective insecticidal agents","authors":"S. A. Abdel-Raheem, A. El-Dean, M. A. A. ul-Malik, R. Hassanien, M. El-sayed, Aly A. Abd-Ella, Sameh A. Zawam, M. Tolba","doi":"10.5267/j.ccl.2021.10.001","DOIUrl":"https://doi.org/10.5267/j.ccl.2021.10.001","url":null,"abstract":"In examining for unique insecticidal agents, two derivatives namely, 2-((3-cyano-4,6-distyrylpyridin-2-yl)thio)-N-(4-nitrophenyl)acetamide (2) and 3-amino-N-(4-nitrophenyl)-4,6-distyrylthieno[2,3-b]pyridine-2-carboxamide (3) were synthesized from distyrylpyridine-2-thione (1). The new compounds were structurally clarified by spectral and elemental analysis data. The insecticidal activity of these compounds were carried out against cowpea aphid, Aphis craccivora Koch. It is demonstrated that the compounds 2 and 3 have noteworthy insecticidal activity against nymphs of cowpea aphid with LC50 values of 0.025-0.027 ppm and 0.005-0.006 ppm after 24 h and 48 h of treatment, respectively. Also, the compounds 2 and 3 have noteworthy insecticidal activity against adults of cowpea aphid with LC50 values of 0.112-0.129 ppm and 0.014-0.015 ppm after 24 h and 48 h of treatment, respectively, that were comparable to that of the control acetamiprid.","PeriodicalId":10942,"journal":{"name":"Current Chemistry Letters","volume":"33 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76400701","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 : 2022-01-01DOI: 10.5267/j.ccl.2022.6.003
A. E. Rhilassi, M. Bennani-Ziatni
The present work investigated the interaction of human insulin with synthesized poorly crystalline apatitic calcium phosphates containing simultaneously HPO42- and CO32- ions in various amount. The adsorption kinetics is very fast, while the release kinetics is generally slow. The chemical composition of apatite has an influence on both the adsorption and release processes. The experimental results show that the percentage of insulin adsorption and release decreased with the increase of the content of carbonate. The equilibrium adsorption data are fitted into Langmuir, Freundlich, Elovich, Temkin, and Dubinin–Radushkevich isotherms. The Langmuir model is best suited with a maximum monolayer adsorption capacity of 33.20 and 25.08 mg/g at 310 K corresponding to the carbonated and octocalcium phosphate apatite respectively. Isotherms parameters have revealed that the adsorption of insulin on these apatites is a feasible, spontaneous, and exothermic process. Fourier-transforms infrared confirm the fixation of insulin on non-carbonated and carbonated apatite. The adsorption and release of insulin molecules can be well described as an ions exchange-reaction between species in the hydrated layer of apatite and other species in solution. All of these results suggested that apatitic calcium phosphates can be used as systems for insulin delivery.
{"title":"Experimental study on the interaction of insulin with apatitic calcium phosphates analogous to bone mineral: adsorption and release","authors":"A. E. Rhilassi, M. Bennani-Ziatni","doi":"10.5267/j.ccl.2022.6.003","DOIUrl":"https://doi.org/10.5267/j.ccl.2022.6.003","url":null,"abstract":"The present work investigated the interaction of human insulin with synthesized poorly crystalline apatitic calcium phosphates containing simultaneously HPO42- and CO32- ions in various amount. The adsorption kinetics is very fast, while the release kinetics is generally slow. The chemical composition of apatite has an influence on both the adsorption and release processes. The experimental results show that the percentage of insulin adsorption and release decreased with the increase of the content of carbonate. The equilibrium adsorption data are fitted into Langmuir, Freundlich, Elovich, Temkin, and Dubinin–Radushkevich isotherms. The Langmuir model is best suited with a maximum monolayer adsorption capacity of 33.20 and 25.08 mg/g at 310 K corresponding to the carbonated and octocalcium phosphate apatite respectively. Isotherms parameters have revealed that the adsorption of insulin on these apatites is a feasible, spontaneous, and exothermic process. Fourier-transforms infrared confirm the fixation of insulin on non-carbonated and carbonated apatite. The adsorption and release of insulin molecules can be well described as an ions exchange-reaction between species in the hydrated layer of apatite and other species in solution. All of these results suggested that apatitic calcium phosphates can be used as systems for insulin delivery.","PeriodicalId":10942,"journal":{"name":"Current Chemistry Letters","volume":"64 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74378886","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 : 2022-01-01DOI: 10.5267/j.ccl.2022.3.003
Fahima Siddikey, Md Abul Hasan Roni, A. Kumer, Unesco Chakma, M. Matin
Natural organic pigments such as carotenoids, betalains, anthocyanins, and carminic acid are notably found as safer food preservatives compared to other harmful synthetic chemicals. Due to glycosylation and acylation, betalains exhibit a broad-spectrum antimicrobial functionality with protection against degenerative diseases. Thus, betalains have been investigated as a potential bacterial inhibitor for food preservative applications. Initially, 36 betalain derivatives have been taken for primary screening using molecular docking. Afterward, the top ten ligands are taken for further study and analysis. The results of Prediction of Activity Spectrum of Substances (PASS) assured the antibacterial capabilities of betalains, and Lipinski's rule-of-five ensures the acceptability of the selected ligands as antibacterial inhibitors. The bacterial pathogens, such as C. botulinum (3FIE), E. coli (2ZWK), and S. typhi (3UU2) are selected for molecular docking by these betalain pigments. Furthermore, ADMET investigations and QSAR studies are performed to check insights into the bacterial inhibition process. Most active and common binding sides were observed at GLY159, ASN165, and SER166 for C. botulinum, at ASP8, LYS40, and TRP50 for E. coli; and at ARG37, GLN5, and ARG74 for S. typhi. The present study clearly shows an excellent insight towards the invention of plant-based new organic inhibitors to face the challenges of bacterial-resistant common food preservatives.
{"title":"Computational investigation of Betalain derivatives as natural inhibitor against food borne bacteria","authors":"Fahima Siddikey, Md Abul Hasan Roni, A. Kumer, Unesco Chakma, M. Matin","doi":"10.5267/j.ccl.2022.3.003","DOIUrl":"https://doi.org/10.5267/j.ccl.2022.3.003","url":null,"abstract":"Natural organic pigments such as carotenoids, betalains, anthocyanins, and carminic acid are notably found as safer food preservatives compared to other harmful synthetic chemicals. Due to glycosylation and acylation, betalains exhibit a broad-spectrum antimicrobial functionality with protection against degenerative diseases. Thus, betalains have been investigated as a potential bacterial inhibitor for food preservative applications. Initially, 36 betalain derivatives have been taken for primary screening using molecular docking. Afterward, the top ten ligands are taken for further study and analysis. The results of Prediction of Activity Spectrum of Substances (PASS) assured the antibacterial capabilities of betalains, and Lipinski's rule-of-five ensures the acceptability of the selected ligands as antibacterial inhibitors. The bacterial pathogens, such as C. botulinum (3FIE), E. coli (2ZWK), and S. typhi (3UU2) are selected for molecular docking by these betalain pigments. Furthermore, ADMET investigations and QSAR studies are performed to check insights into the bacterial inhibition process. Most active and common binding sides were observed at GLY159, ASN165, and SER166 for C. botulinum, at ASP8, LYS40, and TRP50 for E. coli; and at ARG37, GLN5, and ARG74 for S. typhi. The present study clearly shows an excellent insight towards the invention of plant-based new organic inhibitors to face the challenges of bacterial-resistant common food preservatives.","PeriodicalId":10942,"journal":{"name":"Current Chemistry Letters","volume":"37 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81092939","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 : 2022-01-01DOI: 10.5267/j.ccl.2022.4.002
Yulia Matiichuk, Y. Horak, T. Chaban, I. Chaban, V. Matiychuk
By the reaction of (4-furan-2-yl-thiazol-2-yl)- 3a and (4-thiophen-2-yl-thiazol-2-yl)- 3b acetonitriles with furfural 4 and 5-arylfurfyrals 5a-g 3-furan-2-yl-2-(4-furan/thiophen-2-ylthiazol-2-yl)acrylonitrile derivatives 6a-i were obtained. Anticancer activity screening was carried out within the framework of Developmental Therapeutic Program of the National Cancer Institute's (DTP, NCI, Bethesda, Maryland, USA). It was found out that (2E)-3-(2-furyl)-2-[4-(2-furyl)-1,3-thiazol-2-yl]acrylonitrile (6a) and 2-(4-thiophen-2-yl-thiazol-2-yl)-acrylonitriles 6h,i possessed low activity and 2-(4-furan-2-yl-thiazol-2-yl)acrylonitrile derivatives 6b-g showed moderate action. Compounds 6b-g were sensitive to cell lines of MDA-MB-468 and T-47D Breast Cancer. In this case cytotoxic effect was observed with a range of GP = -38.24 – 1.28%.
{"title":"Synthesis and anticancer properties of 3-furan-2-yl-2-(4-furan/thiophen-2-ylthiazol-2-yl)acrylonitrile derivatives","authors":"Yulia Matiichuk, Y. Horak, T. Chaban, I. Chaban, V. Matiychuk","doi":"10.5267/j.ccl.2022.4.002","DOIUrl":"https://doi.org/10.5267/j.ccl.2022.4.002","url":null,"abstract":"By the reaction of (4-furan-2-yl-thiazol-2-yl)- 3a and (4-thiophen-2-yl-thiazol-2-yl)- 3b acetonitriles with furfural 4 and 5-arylfurfyrals 5a-g 3-furan-2-yl-2-(4-furan/thiophen-2-ylthiazol-2-yl)acrylonitrile derivatives 6a-i were obtained. Anticancer activity screening was carried out within the framework of Developmental Therapeutic Program of the National Cancer Institute's (DTP, NCI, Bethesda, Maryland, USA). It was found out that (2E)-3-(2-furyl)-2-[4-(2-furyl)-1,3-thiazol-2-yl]acrylonitrile (6a) and 2-(4-thiophen-2-yl-thiazol-2-yl)-acrylonitriles 6h,i possessed low activity and 2-(4-furan-2-yl-thiazol-2-yl)acrylonitrile derivatives 6b-g showed moderate action. Compounds 6b-g were sensitive to cell lines of MDA-MB-468 and T-47D Breast Cancer. In this case cytotoxic effect was observed with a range of GP = -38.24 – 1.28%.","PeriodicalId":10942,"journal":{"name":"Current Chemistry Letters","volume":"20 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81322509","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 : 2022-01-01DOI: 10.5267/j.ccl.2021.12.001
A. Beheshti, Meghdad Payab, Vahid Seyyed-Ali-Karbasi, Seyyed Amir Siadati
This project was started when an unknown peak was being detected in the organic volatile impurity (OVI) analysis (using the head-space vapor sampling procedure) of bortezomib (BZB) active pharmaceutical ingredient (API), in pharmaceutical companies. During the OVI analysis of the API of BZB, a huge-area peak with an unknown source appeared in the chromatograms of the gas chromatography with flame ionization detector (GC-FID). The data prepared by GC-MAS revealed that the considered huge peak was 3-methylbutanal (3MBut). But, investigating the synthesis procedures showed that during all the synthesis steps, 3MBut or any other solvent containing this impurity was not being applied. Thus, we had concluded that there is a possibility for emergence of this aldehyde from bortezomib itself. To find out which part of bortezomib might turn into 3MBut, we began to investigate all its molecular structure, and hypothesized that the α-amino-boronic acid part of the molecule turned into 3MBut. The experimental analysis and theoretical quantum chemical calculations confirmed that the α-amino-boronic acid center of bortezomib molecule undergoes a rare and unexpected aerobic oxidation by O2 molecule, even in catalyst and solvent-free conditions. The result of this project not only might make clear the passive source of the 3MBut peak of the OVI of bortezomib, but also, it would suggest to store this API in an inert oxygen-free atmosphere to improve the long-term and accelerated (thermal) stability of this very expensive anti-cancer drug.
{"title":"An unexpected aerobic oxidation of α-amino boronic acid part of Borteomib, leading to (thermal) decomposition of this very expensive anti-cancer API","authors":"A. Beheshti, Meghdad Payab, Vahid Seyyed-Ali-Karbasi, Seyyed Amir Siadati","doi":"10.5267/j.ccl.2021.12.001","DOIUrl":"https://doi.org/10.5267/j.ccl.2021.12.001","url":null,"abstract":"This project was started when an unknown peak was being detected in the organic volatile impurity (OVI) analysis (using the head-space vapor sampling procedure) of bortezomib (BZB) active pharmaceutical ingredient (API), in pharmaceutical companies. During the OVI analysis of the API of BZB, a huge-area peak with an unknown source appeared in the chromatograms of the gas chromatography with flame ionization detector (GC-FID). The data prepared by GC-MAS revealed that the considered huge peak was 3-methylbutanal (3MBut). But, investigating the synthesis procedures showed that during all the synthesis steps, 3MBut or any other solvent containing this impurity was not being applied. Thus, we had concluded that there is a possibility for emergence of this aldehyde from bortezomib itself. To find out which part of bortezomib might turn into 3MBut, we began to investigate all its molecular structure, and hypothesized that the α-amino-boronic acid part of the molecule turned into 3MBut. The experimental analysis and theoretical quantum chemical calculations confirmed that the α-amino-boronic acid center of bortezomib molecule undergoes a rare and unexpected aerobic oxidation by O2 molecule, even in catalyst and solvent-free conditions. The result of this project not only might make clear the passive source of the 3MBut peak of the OVI of bortezomib, but also, it would suggest to store this API in an inert oxygen-free atmosphere to improve the long-term and accelerated (thermal) stability of this very expensive anti-cancer drug.","PeriodicalId":10942,"journal":{"name":"Current Chemistry Letters","volume":"97 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85682923","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 : 2022-01-01DOI: 10.5267/j.ccl.2022.5.004
P. J. Kumar, S. Induja, P. Raghavan, B. Gajalakshmi, V. Parthasarathy
The chitosan-coated neem flower powder was prepared and employed as an adsorbent for the removal of cationic methylene blue from an aqueous medium. The interaction of chitosan with neem flower was concluded by FTIR. The BET surface area was evaluated for the prepared NFC adsorbent. The adsorption of methylene blue dye onto chitosan-coated neem flower powder (bio-adsorbent) was carried out by varying the concentration of dye, pH, temperature and concentration of adsorbent. The adsorption capacity was evaluated by using Freundlich and Langmuir models. The adsorption data were further analysed with the help of pseudo-first and second-order kinetic models. The thermodynamic parameters were evaluated to comprehend the nature of the adsorption process.
{"title":"A novel chitosan-coated neem flower bio-adsorbent for the removal of methylene blue dye from wastewater: Thermodynamics, isotherm and kinetic studies","authors":"P. J. Kumar, S. Induja, P. Raghavan, B. Gajalakshmi, V. Parthasarathy","doi":"10.5267/j.ccl.2022.5.004","DOIUrl":"https://doi.org/10.5267/j.ccl.2022.5.004","url":null,"abstract":"The chitosan-coated neem flower powder was prepared and employed as an adsorbent for the removal of cationic methylene blue from an aqueous medium. The interaction of chitosan with neem flower was concluded by FTIR. The BET surface area was evaluated for the prepared NFC adsorbent. The adsorption of methylene blue dye onto chitosan-coated neem flower powder (bio-adsorbent) was carried out by varying the concentration of dye, pH, temperature and concentration of adsorbent. The adsorption capacity was evaluated by using Freundlich and Langmuir models. The adsorption data were further analysed with the help of pseudo-first and second-order kinetic models. The thermodynamic parameters were evaluated to comprehend the nature of the adsorption process.","PeriodicalId":10942,"journal":{"name":"Current Chemistry Letters","volume":"35 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89231798","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 : 2022-01-01DOI: 10.5267/j.ccl.2022.5.001
P. Mondal, S. Mondal
A novel series of spiro cyclo-indolyl β-lactam compounds of the 5-methyl-indole-2,3-dione derivatives has been synthesized from the new Schiff bases Isatin, using the Staudinger synthesis. FT-IR, 1H-NMR, 13C-NMR, mass spectroscopy, and elemental analyses were used to describe the produced chemicals. The anthelmintic potency of the produced compounds was evaluated using standard albendazole. The antibacterial activity also tested for the synthesized compounds by calculating the zone of inhibition using cup plate method and by comparison with the standard Ampicillin against the five different pathogens (Bacillus subtilis (ATCC-1086), Pseudomonas auroginosa (ATCC-1232), Escherichia coli, (ATCC-3273), Proteus mirabilis (ATCC-224), and Staphylococcus aureus (ATCC-449)). The result of anthelmintic potential, when compared to conventional albendazole (PT: 1.324±0.12, DT: 1.421±0.21), synthesized compounds ICP-3B (PT: 1.883±0.24, DT: 1.943±0.02) and ICM-3B (PT: 1.758±0.27, DT: 1.675±0.32) were shown significant activity in terms of paralysis and death time. In the antibacterial study, the compound ICP-3B has shown 20.53mm clear zone of inhibition at 100 µg/mL against the bacteria Bacillus subtilis in comparison to the standard ampicillin (23.04 mm zone). The compound ICM-3B, clearly shows the inhibition zone of 21.27 mm against Bacillus subtilis, 24.64 mm against pseudomonas aeruginosa, 20.62mm against E. coli, 20.41 mm against Proteus mirabilis and 23.65 mm against the bacteria staphylococcus aureus at the level of 100µg/mL. It was confirmed that the compounds were synthesized as expected in the reaction scheme based on the collected spectrum and elemental data. The obtained anthelmintic ant antibacterial results also affirm the potentiality of the synthesized compounds. The further compounds can be synthesised as well as other pharmacological activities can be tested for these compounds with the concept of molecular modelling.
{"title":"Synthesis, characterization and SAR studies of Novel Series of Spiro β-Lactam of 5-methyl-indole-2,3-dione derivatives as a potential antibacterial and anthelmintic agent","authors":"P. Mondal, S. Mondal","doi":"10.5267/j.ccl.2022.5.001","DOIUrl":"https://doi.org/10.5267/j.ccl.2022.5.001","url":null,"abstract":"A novel series of spiro cyclo-indolyl β-lactam compounds of the 5-methyl-indole-2,3-dione derivatives has been synthesized from the new Schiff bases Isatin, using the Staudinger synthesis. FT-IR, 1H-NMR, 13C-NMR, mass spectroscopy, and elemental analyses were used to describe the produced chemicals. The anthelmintic potency of the produced compounds was evaluated using standard albendazole. The antibacterial activity also tested for the synthesized compounds by calculating the zone of inhibition using cup plate method and by comparison with the standard Ampicillin against the five different pathogens (Bacillus subtilis (ATCC-1086), Pseudomonas auroginosa (ATCC-1232), Escherichia coli, (ATCC-3273), Proteus mirabilis (ATCC-224), and Staphylococcus aureus (ATCC-449)). The result of anthelmintic potential, when compared to conventional albendazole (PT: 1.324±0.12, DT: 1.421±0.21), synthesized compounds ICP-3B (PT: 1.883±0.24, DT: 1.943±0.02) and ICM-3B (PT: 1.758±0.27, DT: 1.675±0.32) were shown significant activity in terms of paralysis and death time. In the antibacterial study, the compound ICP-3B has shown 20.53mm clear zone of inhibition at 100 µg/mL against the bacteria Bacillus subtilis in comparison to the standard ampicillin (23.04 mm zone). The compound ICM-3B, clearly shows the inhibition zone of 21.27 mm against Bacillus subtilis, 24.64 mm against pseudomonas aeruginosa, 20.62mm against E. coli, 20.41 mm against Proteus mirabilis and 23.65 mm against the bacteria staphylococcus aureus at the level of 100µg/mL. It was confirmed that the compounds were synthesized as expected in the reaction scheme based on the collected spectrum and elemental data. The obtained anthelmintic ant antibacterial results also affirm the potentiality of the synthesized compounds. The further compounds can be synthesised as well as other pharmacological activities can be tested for these compounds with the concept of molecular modelling.","PeriodicalId":10942,"journal":{"name":"Current Chemistry Letters","volume":"55 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85639219","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 : 2022-01-01DOI: 10.5267/j.ccl.2022.6.001
A. A. Ahmed, S. K. Mohamed, S. A. Abdel-Raheem
Increasing the yield and nutritional value of faba beans is one of the main objectives of the common bean cultivar improvement programs due to its contribution to terminate protein deficiency malnutrition in developing countries and raising the income level of smallholder farmers. In this study, the technological quality of bean seeds from twenty-four genotypes were evaluated (twenty germplasm and four improved cultivars (Misr 1, Giza 429, Giza 716, Giza 843). The results showed a significant diversity in the Egyptian bean germplasm in their quality traits compared to the control cultivars and indicated that the genotypes had a high hydration coefficient that ranged between (98.6-112.4%). While most of the genotypes for cotyledons to hull ratio met the commercial criteria that ranged between (7.41-6.41%). Twenty genotypes had the highest total soluble solids (6.90-11.78%) and were superior to the control cultivars. The seeds chemical composition analysis showed that the genotypes differed in their composition such as protein (26.65 to 30.72 %.), carbohydrate (58.00 to 62.25%), tannin (70.67 to 157.45%), phenols (35.23-51.02 %), and moisture (9.15 to 10.45%).
{"title":"Assessment of the technological quality characters and chemical composition for some Egyptian Faba bean germplasm","authors":"A. A. Ahmed, S. K. Mohamed, S. A. Abdel-Raheem","doi":"10.5267/j.ccl.2022.6.001","DOIUrl":"https://doi.org/10.5267/j.ccl.2022.6.001","url":null,"abstract":"Increasing the yield and nutritional value of faba beans is one of the main objectives of the common bean cultivar improvement programs due to its contribution to terminate protein deficiency malnutrition in developing countries and raising the income level of smallholder farmers. In this study, the technological quality of bean seeds from twenty-four genotypes were evaluated (twenty germplasm and four improved cultivars (Misr 1, Giza 429, Giza 716, Giza 843). The results showed a significant diversity in the Egyptian bean germplasm in their quality traits compared to the control cultivars and indicated that the genotypes had a high hydration coefficient that ranged between (98.6-112.4%). While most of the genotypes for cotyledons to hull ratio met the commercial criteria that ranged between (7.41-6.41%). Twenty genotypes had the highest total soluble solids (6.90-11.78%) and were superior to the control cultivars. The seeds chemical composition analysis showed that the genotypes differed in their composition such as protein (26.65 to 30.72 %.), carbohydrate (58.00 to 62.25%), tannin (70.67 to 157.45%), phenols (35.23-51.02 %), and moisture (9.15 to 10.45%).","PeriodicalId":10942,"journal":{"name":"Current Chemistry Letters","volume":"28 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76176253","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 : 2022-01-01DOI: 10.5267/j.ccl.2022.2.001
A. Abdelgalil, A. A. Mustafa, S. Ali, Omar M. Yassin
Field experiments were carried out for two consecutive seasons at the Experimental Shandaweel Agricultural Research Station, Sohag Governorate, Upper Egypt, during the growing seasons of 2013 and 2014, to study the effect of irrigation intervals and foliar spray of zinc and silicon treatments on chemical composition of maize. Results indicated that scheduling at every 10 days produced the N% , Crude protein%, Cu%, P%, K%, Zn%, Si%, Mn% and Fe% and foliar spray of zinc and silicon treatments produced the highest chemical composition of maize crop. The best N%, Crude protein%, Cu% and Mn were obtained from zinc + silicon treatments followed by zinc, silicon treatments. In contrast, untreated treatments produced the lowest values. It can be concluded that the scheduling at every 10 days and application of foliar spray of zinc + silicon treatments as the effective one could be recommended for scheduling irrigation at every 10 days with application of foliar spray of zinc, silicon or zinc +silicon treatments of maize crop at Shandaweel Agricultural Research Station, Sohag Governorate, Upper Egypt to obtain the best results from chemical composition of maize.
{"title":"Effect of different water deficit and foliar spray of zinc and silicon treatments of chemical composition of maize","authors":"A. Abdelgalil, A. A. Mustafa, S. Ali, Omar M. Yassin","doi":"10.5267/j.ccl.2022.2.001","DOIUrl":"https://doi.org/10.5267/j.ccl.2022.2.001","url":null,"abstract":"Field experiments were carried out for two consecutive seasons at the Experimental Shandaweel Agricultural Research Station, Sohag Governorate, Upper Egypt, during the growing seasons of 2013 and 2014, to study the effect of irrigation intervals and foliar spray of zinc and silicon treatments on chemical composition of maize. Results indicated that scheduling at every 10 days produced the N% , Crude protein%, Cu%, P%, K%, Zn%, Si%, Mn% and Fe% and foliar spray of zinc and silicon treatments produced the highest chemical composition of maize crop. The best N%, Crude protein%, Cu% and Mn were obtained from zinc + silicon treatments followed by zinc, silicon treatments. In contrast, untreated treatments produced the lowest values. It can be concluded that the scheduling at every 10 days and application of foliar spray of zinc + silicon treatments as the effective one could be recommended for scheduling irrigation at every 10 days with application of foliar spray of zinc, silicon or zinc +silicon treatments of maize crop at Shandaweel Agricultural Research Station, Sohag Governorate, Upper Egypt to obtain the best results from chemical composition of maize.","PeriodicalId":10942,"journal":{"name":"Current Chemistry Letters","volume":"76 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2022-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81225176","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}
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