Design, synthesis and antileishmanial in vitro activity of new series of chalcones-like compounds: a molecular hybridization approach

…, JPA Caldas, MR Oliveira, MLAA Vasconcellos

Index: Barbosa, Ticiano P.; Sousa, Suervy C.O.; Amorim, Francianne M.; Rodrigues, Yara K.S.; De Assis, Priscilla A.C.; Caldas, John P.A.; Oliveira, Marcia R.; Vasconcellos, Mario L.A.A. Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 14 p. 4250 - 4256

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Citation Number: 25

Abstract

Abstract The chalcone-like series 1a–1g was efficiently synthesized from Morita–Baylis– Hillman reaction (52–74% yields). Compounds 1a–1g were designed by molecular hybridization based on the anti-inflammatory drug methyl salicylate (3) and the antileishmanial moiety of the Morita–Baylis–Hillman adducts 2a–2g. The 1a–1g compounds were much more actives than precursor series 2a–2g, for example, IC 50= 7.65 μM on ...