PYRROLE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF
申请人:Barth Francis
公开号:US20090281116A1
公开(公告)日:2009-11-12
The invention relates to compounds having the formula (I):
Wherein R
1
, R
2
, R
3
, R
4
, R
5
, R
6
, R
7
and R
9
and A-R
9
are as defined herein. Also disclosed are the preparative methods for the compounds of formula (I) and their use in therapy.
affording E:Z mixtures of alpha,beta-enones. Treatment of the conjugate adducts with PhOH/TMSCl in CH(2)Cl(2) effected carbamate deprotection and cyclization to afford a flexible two-step synthesis of substituted pyrroles.
Nonsteriodal Antiinflammatory Agents, XVII: Inhibition of Bovine Cyclooxygenase and 5-Lipoxygenase byN-Alkyldiphenyl-pyrrolyl Acetic and Propionic Acid Derivatives
作者:G. Dannhardt、M. Lehr
DOI:10.1002/ardp.19933260308
日期:——
A series of 19 N‐alkyl‐diarylpyrrolyl‐acetic and ‐propionicacidderivatives was synthesized and tested. Using bovine blood as enzyme source the inhibition of cyclooxygenase and 5‐lipoxygenase, respectively, was applied to determine the antiinflammatory activity. In general all compounds tested inhibit 5‐lipoxygenase more effectively than cyclooxygenase. A structure‐activity relationship is discussed