3-Methyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester: an exploration of the C-2 position. Part I.

作者信息

Micheli Fabrizio, Di Fabio Romano, Benedetti Roberto, Capelli Anna Maria, Cavallini Palmina, Cavanni Paolo, Davalli Silvia, Donati Daniele, Feriani Aldo, Gehanne Sylvie, Hamdan Mahmoud, Maffeis Micaela, Sabbatini Fabio Maria, Tranquillini Maria Elvira, Viziano Monica Valeria Angela

机构信息

GlaxoSmithKline Medicine Research Centre, via Fleming 4, Verona 37135, Italy.

出版信息

Farmaco. 2004 Mar;59(3):175-83. doi: 10.1016/j.farmac.2003.12.005.

DOI:10.1016/j.farmac.2003.12.005

PMID:14987980

Abstract

Following the recent disclosure of 3-methyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester, a potent and selective mGluR1 non-competitive antagonist, we report here a detailed exploration of the C-2 position of this scaffold with the preparation of differently substituted amides. Great improvement of the pharmacokinetic properties has been achieved through this exercise.

摘要