Synthesis, resolution, and absolute configuration of two novel and selective cyclooxygenase-2 inhibitors based on the 1,5-diarylpyrrole structure

被引:16
作者
Di Bari, Lorenzo
Pescitelli, Gennaro
Salvadori, Piero
Rovini, Michele
Anzini, Maurizio
Cappelli, Andrea
Vomero, Salvatore
机构
[1] Univ Pisa, Dipartimento Chim & Chim Ind, I-56126 Pisa, Italy
[2] Univ Siena, Dipartimento Farmaco Chim Tecnol, I-53100 Siena, Italy
[3] Univ Siena, European Res Ctr Drug Discovery & Dev, I-53100 Siena, Italy
关键词
D O I
10.1016/j.tetasy.2006.12.019
中图分类号
O61 [无机化学];
学科分类号
070301 [无机化学]; 081704 [应用化学];
摘要
Three racemic esters based on the 1,5-diarylpyrrole structure, which proved to be highly selective COX-2 inhibitors endowed with an appreciable anti-inflammatory activity in some animal models, were subjected to chiral resolution. Their absolute configurations were assigned by comparison of the CD spectrum measured on-line with a HPLC-CD detector, with that calculated by means of a TDDFT method. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3430 / 3436
页数:7
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