Synthesis and Biological Evaluation of N- Pyrazolyl Derivatives and Pyrazolopyrimidine Bearing a Biologically Active Sulfonamide Moiety as Potential Antimicrobial Agent

摘要

A series of novel pyrazole-5-carboxylate containing N-triazole derivatives >3,>4; different heterocyclic amines >7a–>b and >10a–>b; pyrazolo[4,3-d]pyrimidine containing sulfa drugs >14a,>b; and oxypyrazolo[4,3-d]pyrimidine derivatives >17, >19, >21 has been synthesized. The structure of the newly synthesized compounds was elucidated on the basis of analytical and spectral analyses. All compounds have been screened for their in vitro antimicrobial activity against three gram-positive and gram-negative bacteria as well as three fungi. The results revealed that compounds >14b and >17 had more potent antibacterial activity against all bacterial strains than reference drug Cefotaxime. Moreover compounds >4, >7b, and >12b showed excellent antifungal activities against Aspergillus niger and Candida albicans in low inhibitory concentrations but slightly less than the reference drug miconazole against Aspergillus flavus.