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

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 pota...

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Veröffentlicht in:Medicinal chemistry research 2012-12, Vol.21 (12), p.4412-4421
Hauptverfasser: Desai, N. C., Pandya, D. D., Satodiya, H. M., Rajpara, K. M., Joshi, V. V., Vaghani, H. V.
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Sprache:eng
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Zusammenfassung: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, 1 H NMR, 13 C 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 μg/mL against selected bacterial strains , while compound 5d , 5f , 5j and 5k were found to be most active with MIC 50  μg/mL against selected fungal strains.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-012-9980-6