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

摘要

A series of fourteen dispiropyrrolidines were synthesized using [3+2]-cycloaddition reactions and were screened for their antimycobacterial activity against Mycobacterium tuberculosis H37Rv in HTS (High Throughput Screen). Most of the compounds showed moderate to good activity with MIC of less than 20 ??M. 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 ??M. ? 2012 Elsevier Ltd. All rights reserved.