Parth P. Patel, Navin B. Patel, Manesh S. Tople, Vatsal M. Patel, Dhanji P. Rajani
{"title":"微波辅助合成2-(芳基烯)-1-噻亚-4-氮杂灵[4.5]decan-3- 1及其抗菌、抗结核和硅筛选","authors":"Parth P. Patel, Navin B. Patel, Manesh S. Tople, Vatsal M. Patel, Dhanji P. Rajani","doi":"10.59467/ijhc.2023.33.285","DOIUrl":null,"url":null,"abstract":"2-(Arylidene)-1-thia-4-azaspiro[4.5]decan-3-ones (3a-e, 4a-e) were synthesized from the 1-thia-4-azaspiro[4.5] decan-3-one through Knoevenagel reaction using the microwave method. In vitro, antibacterial and antitubercular screening of synthetic derivatives 3a-e and 4a-e revealed that compounds 3a and 4b are considerably potent as antibacterial agents against Escherichia coli with MIC = 50 μg/mL and MIC = 50 μg/mL, respectively. Compounds 3e and 4e possessed very good antitubercular activity with MIC = 0.47 μg/mL and MIC = 0.43 μg/mL. The results of molecular docking analysis supported the results of in vitro evaluation as against antibacterial protein compound 3a showed the lowest binding energy and against antitubercular protein, while 3e and 4e were highly attached?","PeriodicalId":54993,"journal":{"name":"Indian Journal of Heterocyclic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.2000,"publicationDate":"2023-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Microwave-Assisted Synthesis of 2-(Arylidene)-1-thia-4-azaspiro[4.5]decan-3-ones and their Antibacterial, Antitubercular, and In Silico Screening\",\"authors\":\"Parth P. Patel, Navin B. Patel, Manesh S. Tople, Vatsal M. Patel, Dhanji P. Rajani\",\"doi\":\"10.59467/ijhc.2023.33.285\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"2-(Arylidene)-1-thia-4-azaspiro[4.5]decan-3-ones (3a-e, 4a-e) were synthesized from the 1-thia-4-azaspiro[4.5] decan-3-one through Knoevenagel reaction using the microwave method. In vitro, antibacterial and antitubercular screening of synthetic derivatives 3a-e and 4a-e revealed that compounds 3a and 4b are considerably potent as antibacterial agents against Escherichia coli with MIC = 50 μg/mL and MIC = 50 μg/mL, respectively. Compounds 3e and 4e possessed very good antitubercular activity with MIC = 0.47 μg/mL and MIC = 0.43 μg/mL. The results of molecular docking analysis supported the results of in vitro evaluation as against antibacterial protein compound 3a showed the lowest binding energy and against antitubercular protein, while 3e and 4e were highly attached?\",\"PeriodicalId\":54993,\"journal\":{\"name\":\"Indian Journal of Heterocyclic Chemistry\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.2000,\"publicationDate\":\"2023-09-30\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Indian Journal of Heterocyclic Chemistry\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.59467/ijhc.2023.33.285\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q4\",\"JCRName\":\"CHEMISTRY, ORGANIC\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Indian Journal of Heterocyclic Chemistry","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.59467/ijhc.2023.33.285","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, ORGANIC","Score":null,"Total":0}
Microwave-Assisted Synthesis of 2-(Arylidene)-1-thia-4-azaspiro[4.5]decan-3-ones and their Antibacterial, Antitubercular, and In Silico Screening
2-(Arylidene)-1-thia-4-azaspiro[4.5]decan-3-ones (3a-e, 4a-e) were synthesized from the 1-thia-4-azaspiro[4.5] decan-3-one through Knoevenagel reaction using the microwave method. In vitro, antibacterial and antitubercular screening of synthetic derivatives 3a-e and 4a-e revealed that compounds 3a and 4b are considerably potent as antibacterial agents against Escherichia coli with MIC = 50 μg/mL and MIC = 50 μg/mL, respectively. Compounds 3e and 4e possessed very good antitubercular activity with MIC = 0.47 μg/mL and MIC = 0.43 μg/mL. The results of molecular docking analysis supported the results of in vitro evaluation as against antibacterial protein compound 3a showed the lowest binding energy and against antitubercular protein, while 3e and 4e were highly attached?
期刊介绍:
Indian Journal of Heterocyclic Chemistry is exclusively devoted to research in the area of heterocyclic chemistry. The journal publishes invited review articles and original research papers pertaining to structure and synthesis, mechanism of reactions, spectral studies, biologically active compounds, bio-chemical studies, physicochemical work, phytochemistry etc.