Synthesis and Biological Activity of 5-(2'-Alkoxycarbonyl substituted phenoxy)furan-2-carboxylic Acid Derivatives

Chia-Lin Chang〈張嘉麟〉 ； Chin-Sheng Wu〈吳錦生〉 ； Sen-Wen Wang〈王賢文〉 ； Jih-Pyang Wang〈王繼平〉

《The Chinese Pharmaceutical Journal》 54卷2期 (2002/04) Pp. 95-113

https://doi.org/10.7019/CPJ.200204.0095

並列摘要

A series of 5-(2’-alkoxycarbonyl substituted phenoxy)furan-2-carboxylic acid derivatives (Id-I2d and Ic-I2c) were prepared by a facile synthetic route: reaction of ethyl 5-nitro-2-furoate (b) with the corresponding salicylates. None of the compounds inhibited PMA-induced neutrophil superoxide formation. On the contrary, some carboxylates, such as compounds 5c and l1c, significantly inhibited fMLP-induced neutrophil degranulation with much greater activity than the positive control, TFP. Compound 5c also inhibited superoxide formation. Furthermore, compound Hc strongly inhibited β-glucuronidase and histamine release from mast cells. In particular, compound Iic was shown to be a novel lead compound with excellent anti-allergic and anti-inflammatory activities. Compound Sc was shown to be a novel lead compound with excellent anti-inflammatory activity.

並列關鍵字

5-(2'-Alkoxycarbonyl substituted phenoxy)furan-2-carboxylic Acid Derivatives； Anti-allergic activity； Anti-inflammatory activity