Journal of Bacteriology & Parasitology

Synthesis, antimalarial and antileishmanial evaluation of some quinazoline derivatives

International Congress on Bacteriology & Infectious Diseases

November 20-22, 2013 DoubleTree by Hilton Baltimore-BWI Airport, MD, USA

Yihenew Simegniew

Accepted Abstracts: J Bacteriol Parasitol

Abstract:

Malaria and leishmaniasis are neglected tropical parasitic diseases affecting billons of people around the globe. Owing to their promising antimalarial and antileishmanial activities, seven novel 2-(substitutedstyryl)-3-aryl-4(3H)-quinazolinones were synthesized in good yields (65.2-86.4%) by using cyclization and condensation reactions. Structures for the synthesized compounds were determined using elemental microanalysis, IR, 1H NMR and 13C NMR (for compound IVb). The in vivo antimalarial and the in vitro antileishmanial activities of the synthesized compounds were evaluated using mice infected with P. berghi ANKA strain and L. donovani strain, respectively. The target compounds showed poor antimalarial activities with percent suppression of 29.10-44.39% which was not significantly different from the negative control group (P>0.05). All the synthesized compounds displayed superior antileishmanial activities (IC50 values, 0.0128-3.1085 μg/ml) as compared to the standard drug miltefosine (IC50=3.1911 μg/ml). (E)-2-(4- chlorostyryl)-3-p-tolyl-4(3H)-quinazolinone (IVb) is the compound with 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.

Biography :

Yihenew Simegniew has completed his BSc degree in chemistry from Bahir Dar University and MSc degree in Medicinal Chemistry from Addis Ababa University at the age of 27 years. He is now working as a lecturer in medicinal chemistry and organic chemistry at Debre Markos University. He has submitted 2 original articles for publication in peer reviewed journal.