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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.