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Synthesis, structure, and bioevaluation of 2,5-bis(arylmethenyl)cyclopentanones.
Liang, Guang; Yang, Shu-Lin; Shao, Li-Li; Zhao, Cheng-Guang; Xiao, Jian; Lv, Yan-Xia; Yang, Ju; Zhao, Yu; Li, Xiao-Kun.
Afiliação
  • Liang G; School of Pharmacy, Wenzhou Medical College, Wenzhou, China.
J Asian Nat Prod Res ; 10(9-10): 957-65, 2008.
Article em En | MEDLINE | ID: mdl-19003615
Curcumin is an excellent lead compound with a variety of bioactivity. Recent articles reported that curcumin's instability and low bioavailability in vivo are mainly due to its easily decomposable beta-diketone moiety. With the aim of bioactive curcumin analogs with better pharmacokinetic property, we present here 11 bis(arylmethenyl)cyclopentanones similar to curcumin and without beta-diketone moiety by reacting relevant arylaldehydes and cyclopentanones. The analogs were structurally determined by 1HNMR and MS spectra, and the crystal structure of 6 was analyzed by X-ray diffraction. Their antibacterial activities in vitro against seven Gram-positive and Gram-negative bacteria were tested, and their inhibition of TNF-alpha and IL-6 secretion in LPS-induced mouse macrophages was investigated using enzyme-linked immunosorbent assay. It was observed that several derivatives displayed higher activity when compared with curcumin, and most of the analogs exhibited activities against the ampicillin-resistant Gram-negative Enterobacter cloacae.
Assuntos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Ciclopentanos Limite: Animals Idioma: En Revista: J Asian Nat Prod Res Assunto da revista: BOTANICA / QUIMICA Ano de publicação: 2008 Tipo de documento: Article País de afiliação: China País de publicação: Reino Unido

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Ciclopentanos Limite: Animals Idioma: En Revista: J Asian Nat Prod Res Assunto da revista: BOTANICA / QUIMICA Ano de publicação: 2008 Tipo de documento: Article País de afiliação: China País de publicação: Reino Unido