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

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

  • Bioorg Med Chem Lett. 2013 Mar 1;23(5):1383-6. doi: 10.1016/j.bmcl.2012.12.069.
Ang Chee Wei 1,  Mohamed Ashraf Ali,  Yeong Keng Yoon,  Rusli Ismail,  Tan Soo Choon,  Raju Suresh Kumar
Affiliations

Affiliation

  • 1 Institute for Research in Molecular Medicine, Universiti Sains Malaysia, Minden 11800, Penang, Malaysia.
PMID: 23352268 DOI: 10.1016/j.bmcl.2012.12.069
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.

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