Synthesis and antimicrobial activity evaluation of pyrazole derivatives containing the imidazo[2,1‐b][1,3,4]thiadiazole moiety

Author:

Qi Jun‐Da1,Meng Yu‐Qing2,Sun Jingxin1,Li Wan‐Xin1,Zhai Hou‐Xiang1,Zhang Changhao1,Quan Jishan12,Jin Cheng‐Hua12ORCID

Affiliation:

1. Key Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy Yanbian University Yanji China

2. Interdisciplinary Program of Biological Function Molecules, College of Integration Science Yanbian University Yanji China

Abstract

AbstractFour series of novel pyrazole derivatives (compounds 17am, 18am, 19ag, and 20ag) were synthesized, and their antibacterial and antifungal activities were evaluated. Most of the target compounds (17am, 18km, and 19bg) showed strong antifungal activity and high selectivity relative to both Gram‐positive and Gram‐negative bacteria. Among them, compounds 17l (minimum inhibitory concentration [MIC] = 0.25 µg/mL) and 17m (MIC = 0.25 µg/mL) showed the strongest antifungal activity, being 2‐ and 4‐fold more active than the positive controls gatifloxacin and fluconazole, respectively. In particular, compound 17l showed little cytotoxicity against human LO2 cells and did not exhibit hemolysis at ultrahigh concentrations, as did the positive control compounds gatifloxacin and fluconazole. These results indicate that these compounds are valuable for further development as antifungal agents.

Funder

National Natural Science Foundation of China

Publisher

Wiley

Subject

Drug Discovery,Pharmaceutical Science

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