Synthesis and evaluation of antibacterial and antimycobacterial activities of some new pyrazole derivatives
JOURNAL OF RESEARCH IN PHARMACY, vol.25, no.5, pp.531-539, 2021 (ESCI, Scopus, TRDizin)
- Publication Type: Article / Article
- Volume: 25 Issue: 5
- Publication Date: 2021
- Doi Number: 10.29228/jrp.43
- Journal Name: JOURNAL OF RESEARCH IN PHARMACY
- Journal Indexes: Emerging Sources Citation Index (ESCI), Scopus, TR DİZİN (ULAKBİM)
- Page Numbers: pp.531-539
- Keywords: Pyrazole, sulfonamide, regioisomer, antibacterial activity, antimycobacterial activity, ANTIMICROBIAL EVALUATION, BIOLOGICAL EVALUATION, DESIGN
- Anadolu University Affiliated: Yes
Abstract
Pyrazoles and sulfonamides are ubiquitously classified as structural fragments in antimicrobial and antimycobacterial agents. In this present study, a series of 14 pyrazole based sulfonamide derivatives (7-20) were designed, synthesized regioisomeric structures were elucidated by spectroscopic methods. All target compounds were evaluated for their in vitro antibacterial potential against selected Gram (+) and Gram (-) bacterial strains as well as for their antimycobacterial activity. The bioactivity results demonstrated that all compounds showed selective antibacterial activity against B. subtilis with MIC values of 1-125 mu g/mL. Especially, 1-[(2,4-dichlorophenyl)methyl]-N-(4- methoxybenzenesulfonyl)-3-methyl-1H-pyrazole-5-carboxamide (9), 14(2,4-Dichlorophenyl)methyll-N-(4- fluorobenzenesulfonyl)-3-methyl-1H-pyrazole-5-carboxamide (10), N-(3,5-Dichlorobenzenesulfonyl)-1-[(2,4- dichlorophenyl)methyl]-3-methyl-1H-pyrazole-5-carboxamide (11) and 1-[(2,4-dichlorophenyl)methyl]-N-(4-fluorobenzenesulfonyl)-5-methyl-1H-pyrazole-3-carboxamide (17) displayed the highest antibacterial activity against B. subtilis with MIC values of 1 mu g/mL, which were more effective compared to the reference chloramphenicol. As a conclusion, the snythesized new pyrazole sulfonamides stand out as promising antimicrobial agents for further development.