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Details van artikel 10 van 17 gevonden artikelen
| Titel: |
Synthesis, structure, and bioevaluation of 2,5-bis(arylmethenyl)cyclopentanones |
| Auteur: |
Liang, Guang Yang, Shu-Lin Shao, Li-Li Zhao, Cheng-Guang Xiao, Jian Lv, Yan-Xia Yang, Ju Zhao, Yu Li, Xiao-Kun |
| Verschenen in: |
Journal of Asian natural products research |
| Paginering: | Jaargang 10 (2008) nr. 10 pagina's 957-965 |
| Jaar: |
2008-10 |
| Inhoud: |
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 β-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 β-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-α 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. |
| Uitgever: |
Taylor & Francis |
| Bronbestand: |
Elektronische Wetenschappelijke Tijdschriften |
Details van artikel 10 van 17 gevonden artikelen
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