An efficient, solvent-free microwave-assisted synthesis and antimicrobial screening of 1,6-dihydropyrimidine analogues

作者：Desai N C^*; Pandya D D; Satodiya H M; Rajpara K M; Joshi V V; Vaghani H V

来源：Medicinal Chemistry Research, 2012, 21(12): 4412-4421.

DOI：10.1007/s00044-012-9980-6

• 1,6-Dihydropyrimidine analogues
• Antimicrobial activity
• Conventional and microwave method
• MIC

A series of compounds 4-(4-(4-aminophenyl)-6-(aryl)-1,6-dihydropyrimidin-2-ylthio)butanenitriles 5a-l were synthesised by the reaction of allyl cyanide 4 with 3a-l. Compounds 3a-l were prepared from reaction between various chalcones 1a-l and thiourea in presence of catalytic amount of potassium hydroxide. Compounds 3a-l, and 5a-l were prepared by classical as well as MWI methods. Structures of the compounds were characterized by IR, H-1 NMR, C-13 NMR and mass spectral data. The newly synthesized compounds 5a-l were screened for their antimicrobial activity against different strains of bacteria and fungi using serial broth dilution method. Compounds 5e, 5g and 5k were found to be most active with MIC of 25 mu g/mL against selected bacterial strains, while compound 5d, 5f, 5j and 5k were found to be most active with MIC 50 mu g/mL against selected fungal strains.

• 出版日期2012-12