2. Academic Validation
  3. A regio- and stereoselective 1,3-dipolar cycloaddition for the synthesis of new-fangled dispiropyrrolothiazoles as antimycobacterial agents

A regio- and stereoselective 1,3-dipolar cycloaddition for the synthesis of new-fangled dispiropyrrolothiazoles as antimycobacterial agents

  • Bioorg Med Chem Lett. 2012 Dec 15;22(24):7418-21. doi: 10.1016/j.bmcl.2012.10.059.
Abdulrahman I Almansour 1,  Sadath Ali,  Mohamed Ashraf Ali,  Rusli Ismail,  Tan Soo Choon,  Velmurugan Sellappan,  Karthi Keyan Elumalai,  Suresh Pandian
Affiliations

Affiliation

  • 1 Department of Chemistry, College of Sciences, King Saud University, PO Box 2455, Riyadh 11451, Saudi Arabia.
PMID: 23122863 DOI: 10.1016/j.bmcl.2012.10.059
Abstract

A series of dispiropyrrolothiazoles compounds were synthesized using 1,3-dipolar cycloaddition and were screened for antimycobacterial activity against Mycobacterium tuberculosis H(37)Rv and INH resistant M. tuberculosis strains. Two of them were showing good activity with MIC of less than 1 μM. Compound (5f) was found to be the most active with MIC of 0.210 and 8.312 μM respectively.

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