A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation
摘要:
In this work, we report a rational structure-based approach aimed at the discovery of new 2-aminoimidazoles as beta-secretase inhibitors. Taking advantage of a microwave-assisted synthetic protocol, a small library of derivatives was obtained and biologically evaluated. Two compounds showed promising activities in both enzymatic and cellular assays. Moreover, one of them exhibited the capability to cross the blood brain barrier as assessed by the parallel artificial membrane permeability assay. (C) 2011 Elsevier Masson SAS. All rights reserved.
Pyrimidone compounds of formula (I):
are inhibitors of the enzyme Lp-PLA2 and are of use in treating atherosclerosis.
公式(I)的嘧啶酮化合物:
是Lp-PLA2酶的抑制剂,并可用于治疗动脉粥样硬化。
[EN] GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES<br/>[FR] ANTAGONISTES VIS-A-VIS DES RECEPTEURS DU GLUCAGON, ELABORATION ET UTILISATIONS THERAPEUTIQUES
申请人:LILLY CO ELI
公开号:WO2005118542A1
公开(公告)日:2005-12-15
The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.