Seifu, Girma Worku (2012) Synthesis of some Novel 2-Styryl-4(3H)-Quinazolinone Derivatives with Potential Antimalarial and Antileishmanial Activities. Masters thesis, Addis Ababa University.
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Abstract
Malaria and leishmaniasis are the most prevalent tropical diseases caused by protozoan parasites. Half of world's population is at risk of malaria and more than 2 million of new cases of leishmaniasis occur annually. There are no effective vaccines available for these diseases and current treatments suffer from several limitations. Therefore, novel drugs for malaria and leishmaniasis are much-needed. In this work, some derivatives of 2-styryl-4(3H)-quinazolinones have been synthesized using different chemical reactions like cyclization, condensation and hydrolysis. The in vivo antimalarial activity of these compounds on P.berghei infected mice was found to be low to moderate with an oral dose of 0.04846 mmol/kg/day. The dose employed for the antimalarial test was equivalent to 25 mg/kg of chloroquine phosphate which causes 100% inhibition of the parasite. Among the synthesized compounds,4-{(1E)-2-[3,4-dihydro-3-(methylphenyl)-4- oxoquinazolin-2-yl]vinyl}-3- methoxyphenyl acetate IVc, showed better activity with percent suppression of 47.44. The other test compounds IVa, IVb, IVd, and Va-Vc exhibited comparable activities. On the other hand, the synthesized compounds were evaluated for their in vitro anti-leishmanial activity against L. donovani. Except for Compounds IVb and IVd which has IC50 value of 3.3248 and 3.3260 μg/ml respectively, the test compounds such as IVa, IVc and Va-Vc (IC50 value 0f 0.0212-2.2654 μg/ml) exhibited better potency than the reference drug miltefosine (IC50 = 3.1911μg/ml). In addition, compound IVa (IC50 = 0.0212 μg/ml) displayed better antileishmanial activity than the reference drug amphotericine B (IC50= 0.0460μg/ml). Compounds IVb-Vc showed less activity than the reference drug amphotericine B.
| Item Type: | Thesis (Masters) |
|---|---|
| Uncontrolled Keywords: | 2-styrylquinazolin-4(3H)-one, in vivo anti-malarial activity, in vitro anti-leishmanial activity and acute toxicity |
| Subjects: | R Medicine > RA Public aspects of medicine > RA0421 Public health. Hygiene. Preventive Medicine R Medicine > RM Therapeutics. Pharmacology R Medicine > RS Pharmacy and materia medica |
| Divisions: | Africana |
| Depositing User: | Emmanuel Ndorimana |
| Date Deposited: | 29 Jun 2018 12:13 |
| Last Modified: | 29 Jun 2018 12:13 |
| URI: | http://thesisbank.jhia.ac.ke/id/eprint/6261 |
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