Objectives:To synthesize a series of novel 3,4-dihydropyrimidine chalcones which has anti-mycobacterial activity and to perform docking studies for active compounds.

Methodology:A series of 6-methyl-4-phenyl-3,4-dihydropyrimidin-2(1H)-one derivatives were synthesized and evaluated their anti-mycobacterial activity against M.tuberculosis H₃₇Rv strain using Micro plate Alamar Blue dye Assay (MABA).

Results: The complete spectral and elemental analytical data of the products, confirmed the formation of novel 6-methyl-4-phenyl-3, 4-dihydropyrimidin-2(1H)-onederivatives. The biological evaluation of all the synthesized compounds against M. tuberculosis H₃₇Rv strain using MABA exhibits one potent compound 6t with MIC value of 3.12 µg/ml and four moderate activity compounds 6a, 6d, 6i and 6q with MIC values of 6.24 µg/ml, 6.24 µg/ml, 12.48 µg/ml and 12.48 µg/ml respectively.

Conclusion: A series of novel dihydropyrimidine chalcones were synthesized, characterized, and evaluated for invitro antimycobacterial H₃₇Rv strain. Compound 6t exhibited potent MIC value compared with reference standard.

Keywords: Antimycobacterial activity,Chalcone, Dihydropyrimidine and MABA.