Design, synthesis, and structure-activity relationships of a series of 3-[2-(1-benzylpiperidin-4-yl) ethylamino] pyridazine derivatives as acetylcholinesterase inhibitors

JM Contreras, I Parrot, W Sippl, YM Rival…

Index: Contreras; Parrot; Sippl; Rival; Wermuth Journal of Medicinal Chemistry, 2001 , vol. 44, # 17 p. 2707 - 2718

Full Text: HTML

Citation Number: 104

Abstract

Starting from the 3-[2-(1-benzylpiperidin-4-yl) ethylamino]-6-phenylpyridazine 1, we performed the design, the synthesis, and the structure-activity relationships of a series of pyridazine analogues acting as AChE inhibitors. Structural modifications were achieved on four different parts of compound 1 and led to the following observations:(i) introduction of a lipophilic environment in the C-5 position of the pyridazine ring is favorable for the AChE- ...