Benzoxazinones as PPARγ agonists. part 1: SAR of three aromatic regions
摘要:
A series of benzoxazinones was synthesized as PPARgamma agonists. The compounds were obtained in seven steps, and SAR was developed by variations to the core shown below. The compounds were tested as functional agonists in the induction of the aP2 gene in preadipocytes, and the most potent compound in the series has an EC50=0.51 muM. The potency was further confirmed through a PPAR-Ga14 construct. Efficacy has been demonstrated in the db/db mouse model of hyperglycemia. (C) 2003 Elsevier Science Ltd. All rights reserved.
[EN] BENZOXAZINE ANTIMICROBIAL AGENTS<br/>[FR] AGENTS ANTIMICROBIENS A BASE DE BENZOXAZINE
申请人:ORTHO PHARMACEUTICAL CORPORATION
公开号:WO1997017333A1
公开(公告)日:1997-05-15
(EN) The invention relates to benzoxazine and pyrido-oxazine antibacterial compounds of general formula (1), wherein the moiety Q is a fused phenyl or fused pyridyl moiety as herein described, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.(FR) L'invention porte sur des composés antimicrobiens de benzoxazine et de pyrido-oxazyne de formule générale (1), dans laquelle la fraction Q est une fraction phényle condensée ou pyridyle condensée telle que spécifiée dans la description, des compositions pharmaceutiques contenant ces composés, leurs procédés de fabrication et leur utilisation dans le traitement des infections bactériennes.
The Preparation of 2-Hydroxyethyl-2,3-dihydro-2h-1,4-benzoxazin-3(4h)-one Derivatives
作者:R. F. Frechette、M. J. Beach
DOI:10.1080/00397919808004455
日期:1998.9
An efficient synthesis of 2-hydroxyethyl-2,3-dihydro-2H-1,4-benzoxazin-3(4H)one derivatives is described using alpha-bromo-gamma-butyrolactone as a bis-electrophile containing a latent hydroxyethyl functional group.