Synthesis and antimicrobial activity of 3-(4-oxo-3,4-dihydrothieno[3,2-d]pyrim- idin-2-yl)propanamides

Abstract

Introduction. The problem of antibiotic resistance is a key topic for modern drug-discovery. Theno- pyrimidine scaffold is considered as a privileged for discovery of antibacterials with diverse suggested mechanism of action starting from bacterial TrmD and N-acetyltransferases to dihydropteroate synthase inhibition. All these mechanisms are promising in tackling of antibiotic resistance. Modification of thienopyrimidine core with the propanoic acid fragment is simple and conveniently produces the series of amides. In this case modification of amide fragment is a flexible instrument for modification of the molecular parameters (e.g. solubility, lipophilicity etc.). We decided to synthesize the series of 3-(4- oxo-3,4-dihydrothieno[3,2-d]pyrimidin-2-yl)propanamides and to test their antimicrobial activity against the standard bacterial strains and a strain of C. albicans.