Green Chemistry Protocol for the Synthesis and Antimycobacterial Activity of Multicomponent Biginelli Condensation Catalyzed by Surfactant in Aqueous Media Beda

Background and Objective: A Simple, Green and efficient procedure for the synthesis of 4-aryl-3, 4-dihydropyrimidine-2(1H)-ones/thione (Biginelli reaction) from 1, 3-dicarbonyl compound, substituted aldehydes and urea/thiourea in the presence of Sodium Dodecyl Sulphate (SDS), a novel catalyst has been introduced in this study. Materials and Methods: The structures of these compounds have been confirmed on the basis of their physical and spectral (IR, HNMR and Mass) data. The dihydropyrimidinone derivatives were evaluated for their in vitro antimycobacterial activity against H37Rv strain by using alamar blue dye method. Results: The synthesized compounds were purified by column chromatography. All the reactions were monitored by TLC and the derivatives were supported by spectral data. The products are obtained in good yield under conventional and domestic microwave methods. All the synthesized compounds exhibited promising activity (MIC: 6.25-100 μg mLG) against Mycobacterium tuberculosis H37Rv. Conclusion: A novel method which is eco-friendly, cost effective, solvent free was developed for the synthesis of dihydropyrimidines under conventional and domestic microwave methods. Using these methods, compounds were produced in high yield. Among 12 compounds screened, IVf found to be most potent with MIC: 6.25 μg mLG with least minimal toxicity some of them were found to possess significant activity, when compared to standard drugs(Streptomycin and Pyrazinamide).