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Background  Leishmaniasis is a neglected tropical parasitic diseases affecting millions of people around the globe. Quinazolines are a group of compounds with diverse pharmacological activities. Owing to their promising antileishmanial activities, some 3-aryl-2-(substitutedstyryl)-4(3 H )-quinazolinones were synthesized in good yields (65.2% to 86.4%).    Results  The target compounds were synthesized by using cyclization, condensation, and hydrolysis reactions. The structures of the synthesized compounds were determined using elemental microanalysis, infrared (IR), and proton nuclear magnetic resonance ( 1 H NMR). The  in vitro  antileishmanial activities of the synthesized compounds were evaluated using  Leishmania donovani  strain. All the synthesized compounds displayed appreciable antileishmanial activities (IC 50  values, 0.0128 to 3.1085 μg/ml) as compared to the standard drug miltefosine (IC 50  = 3.1911 μg/ml). ( E )-2-(4-chlorostyryl)-3- p -tolyl-4(3 H )-quinazolinone ( 7 ) is the compound with the most promising antileishmanial activities (IC 50  = 0.0128 μg/ml) which is approximately 4 and 250 times more active than the standard drugs amphotericin B deoxycholate (IC 50  = 0.0460 μg/ml) and miltefosine (IC 50  = 3.1911 μg/ml), respectively.    Conclusions  The results obtained from this investigation indicate that the synthesized and biologically evaluated quinazoline compounds showed promising antileishmanial activities and are good scaffolds for the synthesis of different antileishmanial agents.    Electronic supplementary material  The online version of this article (doi:10.1186/s13588-014-0010-1) contains supplementary material, which is available to authorized users.

Synthesis and antileishmanial evaluation of some 2,3-disubstituted-4(3H)-quinazolinone derivatives