| Literature DB >> 20855101 |
Cláudio G L Junior1, Priscila A C de Assis, Fábio P L Silva, Suervy C O Sousa, Natália G de Andrade, Ticiano P Barbosa, Patrícia L N Nerís, Luiz V G Segundo, Italo C Anjos, Gabriel A U Carvalho, Gerd B Rocha, Márcia R Oliveira, Mário L A A Vasconcellos.
Abstract
Sixteen aromatic Morita-Baylis-Hillman adducts (MBHA) 1-16 were efficiently synthesized in a one step Morita-Baylis-Hillman reaction (MBHR) involving commercial aldehydes with methyl acrylate or acrylonitrile (81-100% yields) without the formation of side products on DABCO catalysis and at low temperature (0°C). The toxicities of these compounds were assessed against promastigote form of Leishmania amazonensis and Leishmania chagasi. The low synthetic cost of these MBHA, green synthetic protocols, easy one-step synthesis from commercially available and cheap reagents as well as the very good antileishmanial activity obtained for 14 and 16 (IC₅₀ values of 6.88μgmL⁻¹ and 11.06μgmL⁻¹ respectively on L. amazonensis; 9.58μgmL⁻¹ and 14.34μgmL⁻¹ respectively on L. chagasi) indicates that these MBHA can be a novel and promising class of anti-parasitic compounds.Entities:
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Year: 2010 PMID： 20855101 DOI： 10.1016/j.bioorg.2010.08.002
Source DB: PubMed Journal: Bioorg Chem ISSN： 0045-2068 Impact factor: 5.275