Letters in Drug Design & Discovery

Atta-ur-Rahman  , FRS
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: lddd@benthamscience.org

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Synthesis and Antimycobacterial Activity of Highly Functionalised Pyrrolothiazole Derivatives

Author(s): Abdulrahman I. Almansour, Venu Sanjeevi Lakshmipathi, Elumalai Manogaran, Mohamed Ashraf Ali, Farzana Beevi, Tan Soo Choon, Ang Chee Wei, Raju Suresh Kumar and Mohammad Asad

Affiliation: New Drug Discovery Research, Department of Medicinal Chemistry, Alwar Pharmacy College, Alwar, Rajasthan-301030, India.

Keywords: [3+2]-cycloaddition, Antimycobacterial activity, Azomethine ylide, Dispiroheterocycle, Intermolecular.

Graphical Abstract:


Abstract:

A series of twelve pyrralothiazoles was synthesized using [3+2]- cycloaddition reactions. The synthesized compounds were screened for their antimycobacterial activity against M. tuberculosis H37Rv and INH resistant M. tuberculosis strains using agar dilution method, four of them showed good activity with MIC of less than 1µM. Compound (4d) was found to be the most active with MIC of 0.231 µM and 4.372 µM respectively.

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Article Details

VOLUME: 11
ISSUE: 8
Page: [968 - 974]
Pages: 7
DOI: 10.2174/1570180811666140506204239