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作为抗结核分枝杆菌药物的棍状三唑基噻唑新S-衍生物的合成。

Synthesis of new S-derivatives of clubbed triazolyl thiazole as anti-Mycobacterium tuberculosis agents.

作者信息

Shiradkar Mahendra Ramesh, Murahari Kiran Kumar, Gangadasu Hanimi Reddy, Suresh Tatikonda, Kalyan Chakravarthy Akula, Panchal Dolly, Kaur Ranjit, Burange Prashant, Ghogare Jyoti, Mokale Vinod, Raut Mayuresh

机构信息

Dr. Reddy's Laboratories, 7-1-27, Ameerpet, Hyderabad 500016, India.

出版信息

Bioorg Med Chem. 2007 Jun 15;15(12):3997-4008. doi: 10.1016/j.bmc.2007.04.003. Epub 2007 Apr 6.

Abstract

In the present study, a series of N-{4-[(4-amino-5-sulfanyl-4H-1,2,4-triazol-3-yl)methyl]-1,3-thiazol-2-yl}-2-substituted-amide (1a-d) derivatives were synthesized in good yields and characterized by IR, 1H NMR, mass spectral and elemental analyses. The compounds were evaluated for their preliminary in vitro antibacterial activity against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Salmonella typhosa and then were screened for antitubercular activity against Mycobacterium tuberculosis H37 Rv strain by broth microdilution assay method. The antibacterial data of the tested compounds indicated that most of the synthesized compounds showed better activity against bacteria compared to reference drugs. The in vitro antitubercular activity reports of tested compounds against M. tuberculosis strain H37 Rv showed moderate to better activity.

摘要

在本研究中,一系列N-{4-[(4-氨基-5-硫基-4H-1,2,4-三唑-3-基)甲基]-1,3-噻唑-2-基}-2-取代酰胺(1a-d)衍生物以良好的产率合成,并通过红外光谱、1H核磁共振、质谱和元素分析进行表征。对这些化合物针对金黄色葡萄球菌、大肠杆菌、铜绿假单胞菌和伤寒沙门氏菌的初步体外抗菌活性进行了评估,然后通过肉汤微量稀释法筛选其对结核分枝杆菌H37 Rv菌株的抗结核活性。受试化合物的抗菌数据表明,与参考药物相比,大多数合成化合物对细菌表现出更好的活性。受试化合物针对结核分枝杆菌H37 Rv菌株的体外抗结核活性报告显示出中度至较好的活性。

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