Synthesis and in vitro Leishmania promastigote growth inhibition efficacy of novel 4(3H)-quinazolinone derivatives

Abstract

Molecular hybridization is an increasingly important strategy in rational drug design and development. A series of novel quinazolinone-triazole hybrids have been synthesized and their antileishmanial activity investigated. Derivatives (E)-3-(prop-2-yn-1-yl)-2-styrylquinazolin-4(3H)-one, and (E)-3-{[1-(4-bromobenzyl)-1H-1,2,3-triazol4-yl]methyl}-2-styrylquinazolin-4(3H)-one were observed to moderately inhibit the growth of promastigotes. An overall lack of significant antileishmanial activity may be attributable to the poor aqueous solubility of the derivatives. Future research endeavors will focus on potential remediation by investigating the anchoring of hydrophilic moieties to the quinazolinone scaffold.