白脉酸醛的胃细胞保护活性：构效关系

Gastric cytoprotective activity of ilicic aldehyde: structure-activity relationships.

作者信息

Donadel Osvaldo J, Guerreiro Eduardo, María Alejandra O, Wendel Graciela, Enriz Ricardo D, Giordano Oscar S, Tonn Carlos E

机构信息

INTEQUI-CONICET, Facultad de Química, Bioquímica y Farmacia, Universidad Nacional de San Luis, Chacabuco y Pedernera, 5700 San Luis, Argentina.

出版信息

Bioorg Med Chem Lett. 2005 Aug 1;15(15):3547-50. doi: 10.1016/j.bmcl.2005.05.053.

DOI:10.1016/j.bmcl.2005.05.053

PMID:15963720

Abstract

A series of sesquiterpene compounds possessing both eudesmane and eremophilane skeletons were tested as gastric cytoprotective agents on male Wistar rats. The presence of an alpha,beta-unsaturated aldehyde on the C-7 side chain together with a hydroxyl group at C-4 is the requirement for the observed antiulcerogenic activity. In an attempt to establish new molecular structural requirements for this gastric cytoprotective activity, a structure-activity study was performed.

摘要

一系列具有桉叶烷和雅槛蓝烷骨架的倍半萜化合物作为胃细胞保护剂在雄性Wistar大鼠身上进行了测试。C-7侧链上存在α,β-不饱和醛以及C-4上存在羟基是观察到的抗溃疡活性的必要条件。为了确定这种胃细胞保护活性的新分子结构要求，进行了一项构效关系研究。