2. Academic Validation
  3. Antimycobacterial activity: a facile three-component [3+2]-cycloaddition for the regioselective synthesis of highly functionalised dispiropyrrolidines

Antimycobacterial activity: a facile three-component [3+2]-cycloaddition for the regioselective synthesis of highly functionalised dispiropyrrolidines

  • Bioorg Med Chem Lett. 2012 Aug 1;22(15):4930-3. doi: 10.1016/j.bmcl.2012.06.047.
Ang Chee Wei 1,  Mohamed Ashraf Ali,  Yeong Keng Yoon,  Rusli Ismail,  Tan Soo Choon,  Raju Suresh Kumar,  Natarajan Arumugam,  Abdulrahman I Almansour,  Hasnah Osman
Affiliations

Affiliation

  • 1 Institute for Research in Molecular Medicine, Universiti Sains Malaysia, Minden 11800, Penang, Malaysia.
PMID: 22749825 DOI: 10.1016/j.bmcl.2012.06.047
Abstract

A series of twelve dispiropyrrolidines were synthesized using [3+2]-cycloaddition reactions. The synthesized compounds were screened for their antimycobacterial activity against M. tuberculosis H(37)Rv and INH resistant M. tuberculosis strains using agar dilution method, four of them showed good activity with MIC of less than 1 μM. Compound 4'-[5-(4-fluorophenyl)pyridin-3-yl]-1'-methyldispiro[indan-2,2' pyrrolidine-3',2″-indan]-1,3,1″-trione (4b) was found to be the most active with MIC of 0.1215 and 5.121 μM, respectively.

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