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新型 3-取代-N-芳基-6,7-二甲氧基-3a,4-二氢-3H-茚并[1,2-c]吡唑-2-甲酰胺类似物的设计、合成与抗分枝杆菌活性评价。

Design, synthesis and antimycobacterial evaluation of novel 3-substituted-N-aryl-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide analogues.

机构信息

New Drug Discovery Research, Department of Medicinal Chemistry, Alwar Pharmacy College, Alwar, Rajasthan, India.

出版信息

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4451-3. doi: 10.1016/j.bmcl.2011.06.018. Epub 2011 Jun 17.

Abstract

In the present investigation, a series of 3-substituted-N-aryl-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide analogues were synthesized and were evaluated for antitubercular activity by two fold serial dilution technique. All the newly synthesized compounds showed moderate to high inhibitory activities against Mycobacterium tuberculosis H(37)Rv and INH resistant M. tuberculosis. The compound N,3-bis(4-fluorophenyl)-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide (4c) was found to be the most promising compound active against M. tuberculosis H(37)Rv and isoniazid resistant M. tuberculosis with minimum inhibitory concentration 0.78 μM.

摘要

在本研究中,合成了一系列 3-取代-N-芳基-6,7-二甲氧基-3a,4-二氢-3H-茚并[1,2-c]吡唑-2-甲酰胺类似物,并通过两倍系列稀释技术评估了它们的抗结核活性。所有新合成的化合物对结核分枝杆菌 H(37)Rv 和 INH 耐药结核分枝杆菌均显示出中等至高度的抑制活性。化合物 N,3-双(4-氟苯基)-6,7-二甲氧基-3a,4-二氢-3H-茚并[1,2-c]吡唑-2-甲酰胺 (4c) 对结核分枝杆菌 H(37)Rv 和异烟肼耐药结核分枝杆菌的活性最高,最低抑菌浓度为 0.78 μM。

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