Editor-in-Chief Hatice Kübra Elçioğlu Vice Editors Levent Kabasakal Esra Tatar Online ISSN 2630-6344 Publisher Marmara University Frequency Bimonthly (Six issues / year) Abbreviation J.Res.Pharm. Former Name Marmara Pharmaceutical Journal
Journal of Research in Pharmacy 2021 , Vol 25 , Issue 5
Synthesis and evaluation of antibacterial and antimycobacterial activities of some new pyrazole derivatives
Tuğçe GÜR MAZ1,Nursenem KARACA2,Serkan LEVENT3,Burcu ÇALIŞKAN1,Fatih DEMİRCİ4,Erden BANOĞLU1
1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, Ankara, Turkey
2Department of Pharmacognosy, Graduate School of Health Sciences, Anadolu University, Eskisehir, Turkey
3Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskişehir, Turkey
4Department of Pharmacognosy, Faculty of Pharmacy, Anadolu University, Eskişehir, Turkey
5Faculty of Pharmacy, Eastern Mediterranean University, Famagusta, N. Cyprus, Mersin 10, Turkey
DOI : 10.29228/jrp.43 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 μg/mL. Especially, 1-[(2,4-dichlorophenyl)methyl]-N-(4-methoxybenzenesulfonyl)-3-methyl-1H-pyrazole-5-carboxamide (9), 1-[(2,4-Dichlorophenyl)methyl]-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 μg/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. Keywords : Pyrazole; sulfonamide; regioisomer; antibacterial activity; antimycobacterial activity
Marmara University