Ciprofloxacin-isatin-1H-1,2,3-triazole Hybrids: Design, Synthesis, and in vitro Anti-tubercular Activity against M.tuberculosis

被引：30

作者：

Xu, Zhi ^{[1
]}

Lv, Zao-Sheng ^{[1
]}

Song, Xu-Feng ^{[2
]}

Qiang, Min ^{[1
]}

机构：

[1] Wuhan Univ Sci & Technol, Key Lab Hubei Prov Coal Convers & New Carbon Mat, Wuhan, Hubei, Peoples R China

[2] Beijing Univ Technol, Beijing 100124, Peoples R China

来源：

JOURNAL OF HETEROCYCLIC CHEMISTRY | 2018年 / 55卷 / 01期

关键词：

ETHYLENE ISATIN DERIVATIVES; ANTIMYCOBACTERIAL EVALUATION; GATIFLOXACIN;

D O I：

10.1002/jhet.3010

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A new set of ciprofloxacin (CPFX)-isatin-1H-1,2,3-triazole hybrids 6a-l with greater lipophilicity compared with the parent CPFX was designed, synthesized, and assessed for their invitro anti-mycobacterial activity against Mycobacterium tuberculosis (MTB) H(37)Rv as well as cytotoxicity in VERO cell line. The preliminary results showed that all hybrids (MIC: 0.39-50g/mL) exhibited promising activities against MTB H(37)Rv, and six of them (MIC: 0.39-1.56g/mL) were more active than the parent CPFX (MIC: 3.12g/mL). In particular, the most active conjugate 6h (MIC: 0.39g/mL) was comparable with RIF (MIC: 0.39g/mL), and eight times more potent than CPFX. All conjugates (CC50: 4-64g/mL) were more toxic than the parent (CC50: 128g/mL) in VERO cell lines, and the most active hybrids, which also displayed the highest cytotoxicity, should be further optimized.

引用

页码：97 / 102

页数：6

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