4.7 Article

Synthesis and biological evaluation of some novel pyrido[1,2-a] pyrimidin-4-ones as antimalarial agents

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 79, Issue -, Pages 422-435

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.04.031

Keywords

Antimalarial; Plasmodium falcsiparum; Pyrido[1,2-a]pyrimidin-4-one; SYBR Green Assay

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Novel pyrido[1,2-alpha]pyrimidin-4-ones have been synthesized and evaluated for their antimalarial activity by SYBR Green I assay against erythrocytic stages of chloroquine (CQ) sensitive Pf 3D7 strain. The antimalarial screening of 42 different compounds revealed that 3-Fluorobenzyl(4-oxo-4H-pyrido [1,2-alpha] pyrimidin-3-yl)carbamate (21, IC50 value 33 mu M) and 4-Oxo-N[4-(trifluoromethyl)benzy11-4H-pyrido 11,2-alpha]pyrimidine-3-carboxamide (37, IC50 value 37 mu M) showed moderate antimalarial activity. Cytotoxicity study was performed against mammalian cell line (Huh-7) by using the MIT assay for the moderately active compounds. Structural activity relationship (SAR) studies displayed that B-ring unsubstituted pyrido[1,2-alpha]pyrimidine scaffold is responsible for the antimalarial activities of the evaluated derivatives. This SAR based antimalarial screening supported that pyrido[1,2-alpha]pyrimidin-4-one can be considered as a lead heterocyclic structure for further development of more potent derivatives for antimalarial activity.(c) 2014 Elsevier Masson SAS. All rights reserved.

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