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发现新型甲酮衍生物作为抗分枝杆菌剂。

Discovery of novel methanone derivatives acting as antimycobacterial agents.

机构信息

Pharmacogenetic and Novel Therapeutics Research, Institute for Research in Molecular Medicine, Universiti of Sains Malaysia, Pennag, Malaysia.

出版信息

J Enzyme Inhib Med Chem. 2011 Dec;26(6):890-4. doi: 10.3109/14756366.2011.559945. Epub 2011 Mar 14.

Abstract

A series of pyrazoline derivatives were synthesized and in vitro activity against Mycobacterium tuberculosis H37Rv was carried out. Among the synthesized compounds, compounds (4d) and (4f) 4-aminophenyl-3-(3,4-dimethoxyphenyl)-6,7-dimethoxy-2,3,3a,4-tetrahydroindeno[1,2-c]pyrazol-2-ylmethanone and 4-aminophenyl-6,7-dimethoxy-3-phenyl-2,3,3a,4-tetrahydroindeno[1,2-c]pyrazol-2-ylmethanone were found to be the most active agent against M. tuberculosis H37Rv with a minimum inhibitory concentration of 10 μg/mL.

摘要

合成了一系列吡唑啉衍生物,并对其进行了体外抗结核分枝杆菌 H37Rv 的活性测试。在所合成的化合物中,化合物(4d)和(4f)4-氨基苯基-3-(3,4-二甲氧基苯基)-6,7-二甲氧基-2,3,3a,4-四氢茚并[1,2-c]吡唑-2-基甲酮和 4-氨基苯基-6,7-二甲氧基-3-苯基-2,3,3a,4-四氢茚并[1,2-c]吡唑-2-基甲酮对结核分枝杆菌 H37Rv 的活性最强,最小抑菌浓度为 10μg/mL。

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