Unsymmetrical 1,5-diaryl-3-oxo-1,4-pentadienyls and their evaluation as antiparasitic agents
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- 作者：Zia Ud Din ; Taicia Pacheco Fill ; Francisco Favaro de Assis ; Danielle Lazarin-Bid贸ia ; Vanessa Kaplum ; Francielle Pelegrin Garcia ; Celso Vataru Nakamura ; Kleber Thiago de Oliveira ; Edson Rodrigues-Filho
- 关键词：Dibenzalacetone ; Chalcone analogues ; Curcumin analogues ; 1 ; 5-Diaryl-3-oxo-1 ; 4-pentadienyl ; Leishmania ; Trypanosoma
- 刊名：Bioorganic and Medicinal Chemistry
- 出版年：1 February, 2014
- 年：2014
- 卷：22
- 期：3
- 页码：1121-1127
- 全文大小：521 K
文摘
In this work the synthesis and antiparasitical activity of new 1,5-diaryl-3-oxo-1,4-pentadienyl derivatives are described. First, compounds 1a, 1b, 1c and 1d were prepared by acid-catalyzed aldol reaction between 2-butanone and benzaldehyde, anisaldehyde, p-N,N-dimethylaminobenzaldehyde and p-nitrobenzaldehyde. Reacting each of the methyl ketones 1a, 1b, 1c and 1d with the p-substituted benzaldehydes under basic-catalyzed aldol reaction, we further prepared compounds 2a-2p. All twenty compounds were evaluated for antiproliferative activity, particularly for promastigote of Leishmania amazonensis and epimastigote of Trypanosoma cruzi. All compounds showed good activity while nitro compounds 2i and 2k showed inhibition activity at a few 渭M.