Discovery of novel N-acylsulfonamide analogs as potent and selective EP3 receptor antagonists
摘要:
A series of novel N-acylsulfonamide analogs were synthesized and evaluated for their binding affinity and antagonist activity for the EP3 receptor subtype. Representative compounds were also evaluated for their inhibitory effect on PGE(2)-induced uterine contraction in pregnant rats. Among those tested, a series of N-acylbenzenesulfonamide analogs were found to be more potent than the corresponding carboxylic acid analogs in both the in vitro and in vivo evaluations. The structure activity relationships (SAR) are also discussed. (C) 2010 Published by Elsevier Ltd.
Compounds of formula (I)
as well as pharmaceutically acceptable salts and esters thereof, wherein L, R
1
, R
2
, m and n have the meaning given in claim
1
and which can be used in the form of pharmaceutical compositions.
公式(I)的化合物,以及 pharmaceutically acceptable salts and esters thereof,其中 L, R1, R2, m 和 n 的含义如权利要求 1 所述,并且可以以药物组合物的形式使用。
A mild, efficient method for the synthesis of aromatic and aliphatic sulfonamides
作者:Wing Yan Chan、Carl Berthelette
DOI:10.1016/s0040-4039(02)00848-1
日期:2002.6
two-step method was developed for the synthesis of aromatic and aliphatic sulfonamides from the corresponding sulfinates using bis(2,2,2-trichloroethyl)azodicarboxylate as the electrophilic nitrogen source. The intermediate sulfonylhydrazides were obtained in very good yields and were cleaved under reductive conditions to deliver the desired sulfonamides. A variety of substituents in the aromatic ring