Abstract
BackgroundLeishmaniasis 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(3H)-quinazolinones were synthesized in good yields (65.2% to 86.4%).ResultsThe 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 (1H NMR). The in vitro antileishmanial activities of the synthesized compounds were evaluated using Leishmania donovani strain. All the synthesized compounds displayed appreciable antileishmanial activities (IC50 values, 0.0128 to 3.1085 μg/ml) as compared to the standard drug miltefosine (IC50 = 3.1911 μg/ml). (E)-2-(4-chlorostyryl)-3-p-tolyl-4(3H)-quinazolinone (7) is the compound with the most promising antileishmanial activities (IC50 = 0.0128 μg/ml) which is approximately 4 and 250 times more active than the standard drugs amphotericin B deoxycholate (IC50 = 0.0460 μg/ml) and miltefosine (IC50 = 3.1911 μg/ml), respectively.ConclusionsThe 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 materialThe online version of this article (doi:10.1186/s13588-014-0010-1) contains supplementary material, which is available to authorized users.
Highlights
Leishmaniasis is a neglected tropical parasitic diseases affecting millions of people around the globe
Infrared (IR) spectra in nujol were recorded with the SHIMADZU 8400SP FT-IR spectrophotometer (Shimadzu Corporation, Nakagyo-ku, Kyoto, Japan), and proton nuclear magnetic resonance (1H NMR) spectral data were performed on Bruker Avance DMX400 FT-NMR spectrometer (Bruker, Billerica, MA, USA) using tetramethyl silane (TMS) as internal standard
The target compounds are synthesized in a good yield, which ranged from 65.2% to 86.4% (Table 1)
Summary
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(3H)-quinazolinones were synthesized in good yields (65.2% to 86.4%). Leishmanisis is a neglected tropical disease resulting from infection of macrophages by obligate intracellular parasites of the genus Leishmania [1,2,3]. It is a public health problem in at least 88 countries with an estimated 350 million people at risk. 1.5 to 2 million new cases and 70,000 deaths occur due to cutaneous leishmaniasis (CL). The number of cases of leishmaniasis is increasing globally due to Leishmania/HIV co-infection [5,6], international travel, and migration of immigrants and refugees from endemic regions [7,8]
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