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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
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.
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页码:496 / 500
页数:5
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