Study of antileishmanial activity of 2-aminobenzoyl amino acid hydrazides and their quinazoline derivatives |
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| Authors: | Sherine Nabil Khattab Nesreen Saied Haiba Ahmed Mosaad Asal Adnan A Bekhit Aida A Guemei Adel Amer Ayman El-Faham |
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| Institution: | 1. Department of Chemistry, Faculty of Science, Alexandria University, P.O. Box 426, Ibrahimia, Alexandria 21321, Egypt;2. Department of Physics and Chemistry, Faculty of Education, Alexandria University, Egypt;3. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Alexandria University, Alexandria 21521, Egypt;4. Department of Clinical Pharmacology, Faculty of Medicine, University of Alexandria, Alexandria, Egypt;5. Department of Applied Chemistry, Faculty of Applied Science, Taibah University, Saudi Arabia;6. Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, Riyadh 11451, Saudi Arabia |
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| Abstract: | A new small library of 2-aminobenzoyl amino acid hydrazide derivatives and quinazolinones derivatives was synthesized and fully characterized by IR, NMR, and elemental analysis. The activity of the prepared compounds on the growth of Leishmania aethiopica promastigotes was evaluated. 2-Benzoyl amino acid hydrazide showed higher inhibitory effect than the quinazoline counterpart. The in vitro antipromastigote activity demonstrated that compounds 2a, 2b, 2f and 4a had IC50 better than standard drug miltefosine and comparable activity to amphotericin B deoxycholate, which indicates their high antileishmanial activity against Leishmania. aethiopica. Among the prepared compounds; 2-amino-N-(6-hydrazinyl-6-oxohexyl)benzamide 2f (IC50 = 0.051 μM) has the best activity, 154 folds more active than reference standard drug miltefosine (IC50 = 7.832 μM), and half fold the activity of amphotericin B (IC50 = 0.035 μM). In addition, this compound was safe and well tolerated by experimental animals orally up to 250 mg/kg and parenterally up to 100 mg/kg. |
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| Keywords: | Amino acid hydrazides Quinazolinones Antileishmanial activity |
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