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一种简便的三组分[3+2]环加成反应，用于高区域选择性合成作为抗分枝杆菌剂的高度官能化的双吡咯烷。

A facile three-component [3+2]-cycloaddition for the regioselective synthesis of highly functionalised dispiropyrrolidines acting as antimycobacterial agents.

机构信息

Institute for Research in Molecular Medicine, Universiti Sains Malaysia, Minden 11800, Penang, Malaysia.

出版信息

Bioorg Med Chem Lett. 2013 Mar 1;23(5):1383-6. doi: 10.1016/j.bmcl.2012.12.069. Epub 2013 Jan 4.

DOI:10.1016/j.bmcl.2012.12.069
PMID:23352268
Abstract

A series of fourteen dispiropyrrolidines were synthesized using [3+2]-cycloaddition reactions and were screened for their antimycobacterial activity against Mycobacterium tuberculosis H(37)Rv in HTS (High Throughput Screen). Most of the compounds showed moderate to good activity with MIC of less than 20 μM. Compound 4'-(4-bromophenyl)-1'-methyldispiro[acenaphthylene-1,2'-pyrrolidine-3',2″-indane]-2,1″(1H)-dione (4c) was found to be the most active with MIC of 12.50 μM.

摘要

合成了一系列 14 个双吡咯烷，并通过高通量筛选（HTS）对其抗结核分枝杆菌 H(37)Rv 的活性进行了筛选。大多数化合物表现出中等至良好的活性，MIC 小于 20 μM。化合物 4'-(4-溴苯基)-1'-甲基二螺[吖啶-1,2'-吡咯啶-3',2″-茚]-2,1″(1H)-二酮（4c）表现出最高的活性，MIC 为 12.50 μM。

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