Pub Date : 2021-10-07DOI: 10.56042/ijcb.v60i8.30478
Yufei Li, Lan Jiang, Li Zhang, Jingyu Wang, Peng Xiang, J. Pan, Xiangnan Hu
Efficient and high yielding methods for the preparation of vildagliptin 1 intermediate of (S)-1-(2-chloroacetyl) pyrrolidine-2-carbonitrile 2 and 3-amino-1-adamantane alcohol 3 respectively have been described. (S)-1-(2-Chloroacetyl) pyrrolidine-2-carbonitrile 2 has been synthesized from L-proline 2a via chloroacetyl chloride, performed with acetonitrile in the presence of sulfuric acid via one-pot reactions. 3-Amino-1-adamantane alcohol 3 has been prepared from amantadine hydrochloride via oxidation by sulfuric acid/nitric acid and boric acid as catalyst, and has been subjected to ethanol extraction. The overall yield is about 95%.
{"title":"An efficient synthesis of Vildagliptin intermediates","authors":"Yufei Li, Lan Jiang, Li Zhang, Jingyu Wang, Peng Xiang, J. Pan, Xiangnan Hu","doi":"10.56042/ijcb.v60i8.30478","DOIUrl":"https://doi.org/10.56042/ijcb.v60i8.30478","url":null,"abstract":"Efficient and high yielding methods for the preparation of vildagliptin 1 intermediate of (S)-1-(2-chloroacetyl) pyrrolidine-2-carbonitrile 2 and 3-amino-1-adamantane alcohol 3 respectively have been described. (S)-1-(2-Chloroacetyl) pyrrolidine-2-carbonitrile 2 has been synthesized from L-proline 2a via chloroacetyl chloride, performed with acetonitrile in the presence of sulfuric acid via one-pot reactions. 3-Amino-1-adamantane alcohol 3 has been prepared from amantadine hydrochloride via oxidation by sulfuric acid/nitric acid and boric acid as catalyst, and has been subjected to ethanol extraction. The overall yield is about 95%.","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":"8 1","pages":""},"PeriodicalIF":0.5,"publicationDate":"2021-10-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77649431","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}
Pub Date : 2021-10-07DOI: 10.56042/ijcb.v60i8.30912
A. Kumar, V. Sunithab, P. Shankaraiaha, P. Jalapathic
A Kishore Kumar*, V Sunitha, P Shankaraiah & P Jalapathi a Department of Humanities and Sciences, Vardhaman College of Engineering, Shamshabad, Hyderabad 501 218, India b Department of Chemistry, University College of Science, Osmania University, Saifabad, Hyderabad 500 004, India c Department of Chemistry, University College of Engineering, Osmania University, Hyderabad 500 007, India E-mail: kishoreangajala@gmail.com
A Kishore Kumar*， V Sunitha, P Shankaraiah & P Jalapathi A Vardhaman工程学院人文科学系，沙姆沙巴德，海得拉巴501 218，印度b大学理学院化学系，海得拉巴500004，印度c大学工程学院化学系，海得拉巴500007，印度E-mail: kishoreangajala@gmail.com
{"title":"Synthesis, characterization and antimicrobial evaluation of some novel (3-methyl-5-((3-phenylisoxazol-5-yl)methoxy)benzofuran-2-yl)(phenyl)methanones","authors":"A. Kumar, V. Sunithab, P. Shankaraiaha, P. Jalapathic","doi":"10.56042/ijcb.v60i8.30912","DOIUrl":"https://doi.org/10.56042/ijcb.v60i8.30912","url":null,"abstract":"A Kishore Kumar*, V Sunitha, P Shankaraiah & P Jalapathi a Department of Humanities and Sciences, Vardhaman College of Engineering, Shamshabad, Hyderabad 501 218, India b Department of Chemistry, University College of Science, Osmania University, Saifabad, Hyderabad 500 004, India c Department of Chemistry, University College of Engineering, Osmania University, Hyderabad 500 007, India E-mail: kishoreangajala@gmail.com","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":"22 1","pages":""},"PeriodicalIF":0.5,"publicationDate":"2021-10-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74131750","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}
Pub Date : 2021-10-07DOI: 10.56042/ijcb.v60i8.27844
{"title":"Designing a new vanillin Schiff base (Z)-4-((2-hydroxy-3-methoxy benzylidene)amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one: Synthesis, characterization, crystal structure and biological studies","authors":"","doi":"10.56042/ijcb.v60i8.27844","DOIUrl":"https://doi.org/10.56042/ijcb.v60i8.27844","url":null,"abstract":"","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":"105 1","pages":""},"PeriodicalIF":0.5,"publicationDate":"2021-10-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76140874","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}
Pub Date : 2021-10-07DOI: 10.56042/ijcb.v60i8.30157
{"title":"Synthesis and biological activity of 7-(2-(1H-1,2,4-triazol-1-yl)ethoxy)-4-(styryl/4-substituted styryl)-2H-chromen-2-one","authors":"","doi":"10.56042/ijcb.v60i8.30157","DOIUrl":"https://doi.org/10.56042/ijcb.v60i8.30157","url":null,"abstract":"","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":"31 1","pages":""},"PeriodicalIF":0.5,"publicationDate":"2021-10-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83158312","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}
Pub Date : 2021-10-07DOI: 10.56042/ijcb.v60i8.29194
A. M. Alraih, M. A. Mohamed, M. Alansari, A. Osman, K. Ahmed, Ayda Y. Abdelrahman, M. Hamid
Acacia species (Mimosaceae) is widely distributed in tropical and subtropical countries and has a variety of ethnomedicinal uses. There is inadequate laboratory investigation to identify bioactive compounds and therapeutic effect of Acacia nilotica var. adstringens. This research was conducted to extract, isolate and identify major compounds from heartwood of Acacia nilotica var. adstringens and to test them against representative bacteria. Powdered air-dried heartwood of A. nilotica var. adstringens was extracted with methanol/water, 4:1 and the extracted was then purified using chromatographic techniques (column and paper chromatography). A pure flavonoid compound was isolated and the structure was elucidated based on extensive spectroscopic analysis procedures (IR, UV, 1H-NMR, and MS spectrometery). The isolated compound was then evaluated for antimicrobial potential against Gram-negative (Escherichia coli and Pseudomonas aeruginosa) and Gram-positive bacteria (Bacillus subtilis, Bacillus cereus, and Staphylococcus aureus) using cub-plate agar diffusion method. The spectroscopic analysis of the isolated compound led to its identification as 7, 3`, 4`-trihydroxyflavonol. The compound showed varying antimicrobial responses with high potency against Gram-negative human pathogens. The Gram-positive bacteria which were inhibited were Bacillus cereus, Corynebacterium sp., Enterococcus faecalis, Staphylococcus aureus, and Streptococcus agalactiae. The Gram-negative bacteria were Acinetobacter baumannii, Acinetobacter sp., Escherichia coli, Pseudomonas aeruginosa and yeasts were Candida albicans and Cryptococcus neoformans. The present study demonstrated that 7, 3`, 4`-trihydroxyflavonol is an effective antimicrobial compound. If applied in suitable pharmaceutical formulations it could be valuable for treating various bacterial infections or introduced as adjunct treatment along with standard agents.
{"title":"Antimicrobial activity of 7,3ʹ,4ʹ-trihydroxyflavonol isolated from Acacia nilotica var. ad stringens","authors":"A. M. Alraih, M. A. Mohamed, M. Alansari, A. Osman, K. Ahmed, Ayda Y. Abdelrahman, M. Hamid","doi":"10.56042/ijcb.v60i8.29194","DOIUrl":"https://doi.org/10.56042/ijcb.v60i8.29194","url":null,"abstract":"Acacia species (Mimosaceae) is widely distributed in tropical and subtropical countries and has a variety of ethnomedicinal uses. There is inadequate laboratory investigation to identify bioactive compounds and therapeutic effect of Acacia nilotica var. adstringens. This research was conducted to extract, isolate and identify major compounds from heartwood of Acacia nilotica var. adstringens and to test them against representative bacteria. Powdered air-dried heartwood of A. nilotica var. adstringens was extracted with methanol/water, 4:1 and the extracted was then purified using chromatographic techniques (column and paper chromatography). A pure flavonoid compound was isolated and the structure was elucidated based on extensive spectroscopic analysis procedures (IR, UV, 1H-NMR, and MS spectrometery). The isolated compound was then evaluated for antimicrobial potential against Gram-negative (Escherichia coli and Pseudomonas aeruginosa) and Gram-positive bacteria (Bacillus subtilis, Bacillus cereus, and Staphylococcus aureus) using cub-plate agar diffusion method. The spectroscopic analysis of the isolated compound led to its identification as 7, 3`, 4`-trihydroxyflavonol. The compound showed varying antimicrobial responses with high potency against Gram-negative human pathogens. The Gram-positive bacteria which were inhibited were Bacillus cereus, Corynebacterium sp., Enterococcus faecalis, Staphylococcus aureus, and Streptococcus agalactiae. The Gram-negative bacteria were Acinetobacter baumannii, Acinetobacter sp., Escherichia coli, Pseudomonas aeruginosa and yeasts were Candida albicans and Cryptococcus neoformans. The present study demonstrated that 7, 3`, 4`-trihydroxyflavonol is an effective antimicrobial compound. If applied in suitable pharmaceutical formulations it could be valuable for treating various bacterial infections or introduced as adjunct treatment along with standard agents.","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":"15 1","pages":""},"PeriodicalIF":0.5,"publicationDate":"2021-10-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90877372","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}
Pub Date : 2021-10-07DOI: 10.56042/ijcb.v60i8.30567
{"title":"Biological evaluation of some novel chalcones and their derivatives","authors":"","doi":"10.56042/ijcb.v60i8.30567","DOIUrl":"https://doi.org/10.56042/ijcb.v60i8.30567","url":null,"abstract":"","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":"43 1","pages":""},"PeriodicalIF":0.5,"publicationDate":"2021-10-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74084579","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}
Pub Date : 2021-10-05DOI: 10.56042/ijcb.v60i7.44455
{"title":"Synthesis of N-aminoimidazol-2-thione derivatives using tandem approach","authors":"","doi":"10.56042/ijcb.v60i7.44455","DOIUrl":"https://doi.org/10.56042/ijcb.v60i7.44455","url":null,"abstract":"","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":"126 1","pages":""},"PeriodicalIF":0.5,"publicationDate":"2021-10-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79179803","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}
Pub Date : 2021-10-05DOI: 10.56042/ijcb.v60i7.29363
{"title":"Synthesis, characterization and antimicrobial activity of some novel 1-amino dibenzofuran derivatives","authors":"","doi":"10.56042/ijcb.v60i7.29363","DOIUrl":"https://doi.org/10.56042/ijcb.v60i7.29363","url":null,"abstract":"","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":"1 1","pages":""},"PeriodicalIF":0.5,"publicationDate":"2021-10-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76016281","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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