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Arch Pharm (Weinheim). 2019 Oct;352(10):e1900135. doi: 10.1002/ardp.201900135. Epub 2019 Aug 22.

Gatifloxacin-1,2,3-triazole-isatin hybrids and their antimycobacterial activities.

Author information

1
Department of Pharmacy, Bozhou People's Hospital, Bozhou, China.
2
Department of Clinical Laboratory, Lianshui County People's Hospital, Lianshui, China.
3
School of Nuclear Technology and Chemistry and Biology, Hubei University of Science and Technology, Xianning, China.

Abstract

A series of gatifloxacin-1,2,3-triazole-isatin hybrids 8a-l were designed, synthesized, and screened for their in vitro antimycobacterial activity as well as cytotoxicity toward Chinese Hamster Ovary (CHO) cells. The synthesized hybrids showed considerable activity against MTB H37 Rv and two MDR-MTB strains with minimal inhibitory concentration (MIC) of 0.25-8 μg/ml, and the hybrid 8a (MICMTB H37Rv : 0.25 μg/ml and MICMDR-MTB : 0.5 and 1 μg/ml) was found to be most active against the tested strains, which was not inferior to the parent gatifloxacin (MIC: 0.5, 0.25, and 0.5 μg/ml) against all three tested strains, and was ≥128-fold more active than isoniazid (MIC: ≥64 μg/ml) and rifampicin (MIC: >128 μg/ml) against the two MDR-MTB strains. Moreover, hybrid 8a (CC50 : 8.0 μg/ml) also displayed acceptable cytotoxicity toward CHO cells, and the selectivity index was 32. The structure-activity relationship and structure-cytotoxicity relationship were also enriched.

KEYWORDS:

1,2,3-triazole; antimycobacterial; antitubercular; gatifloxacin; isatin; multidrug resistant

PMID:
31441087
DOI:
10.1002/ardp.201900135

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