Design, synthesis, and in vitro antituberculosis activity of benzo[6,7]cyclohepta[1,2-b]pyridine-1,3,4-oxadiazole derivatives

被引：9
作者：
Sajja, Yasodakrishna [1 ]
Vanguru, Sowmya [1 ]
Vulupala, Hanmanth Reddy [1 ]
Nagarapu, Lingaiah [1 ]
Perumal, Yogeswari [2 ]
Sriram, Dharmarajan [2 ]
Nanubolu, Jagadeesh Babu [3 ]
机构：
[1] CSIR Indian Inst Chem Technol, Organ Chem Div CPC 2, Hyderabad, Telangana, India
[2] Birla Inst Technol & Sci Pilani, Pharm Grp, Med Chem & Antimycobacterial Res Lab, Hyderabad, Telangana, India
[3] CSIR Indian Inst Chem Technol, Ctr Xray Crystallog, Hyderabad, Telangana, India
来源：
CHEMICAL BIOLOGY & DRUG DESIGN | 2017年 / 90卷 / 04期
关键词：
1; 3; 4-oxadiazoles; benzo[6; 7]cyclohepta[1; 2-b]pyridine; cytotoxicity; di(acetoxy)iodobenzene; Mycobacterium tuberculosis; POTENTIAL ANTICANCER AGENTS; ANTIINFLAMMATORY ACTIVITY; BIOLOGICAL EVALUATION; EFFICIENT SYNTHESIS; TUBERCULOSIS; DESLORATADINE; INHIBITORS; DRUGS; TB;
D O I：
10.1111/cbdd.12969
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
A new antitubercular agents, benzo[6,7]cyclohepta[1,2-b]pyridine-1,3,4- oxadiazole hybrids (6a-o), have been designed and synthesized involving oxidative cyclization of hydrazones by use of di(acetoxy)iodobenzene, characterized by IR,H-1 NMR,C-13 NMR, and HRMS, and further confirmed by X-ray analysis. All the newly synthesized compounds 4a-o evaluated for their in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv (ATCC27294). Among the compounds tested, the compounds 4o (MIC: 1.56g/ml) and 4l, 4m (MIC: 3.125g/ml) are promising lead analogues and have shown lower cytotoxicity.
引用
收藏
页码：496 / 500
页数：5
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