title: Synthesis and antileishmanial evaluation of some 2,3-disubstituted-4(3H)-quinazolinone derivatives.
abstract: 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(3H)-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 (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.
  
  
  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.
authors.affiliation: Department of Chemistry, Natural and Computational Science College, Debre Markos University, Debre Markos, Ethiopia. yihenews@gmail.com.
authors.forename: Yihenew Simegniew
authors.initials: YS
authors.lastname: Birhan
authors.affiliation: Department of Pharmaceutical Chemistry, Alexandria University, Alexandria, 21215, Egypt. adnbekhit@yahoo.com.
authors.forename: Adnan Ahmed
authors.initials: AA
authors.lastname: Bekhit
authors.affiliation: Department of Pharmaceutical Chemistry and Pharmacognosy, School of Pharmacy, Addis Ababa University, Addis Ababa, Ethiopia. hymete@yahoo.com.
authors.forename: Ariaya
authors.initials: A
authors.lastname: Hymete
keywords: Antileishmanial activities; Leishmania; Quinazolinones