Literature DB >> 14987980

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.

Fabrizio Micheli1, Romano Di Fabio, Roberto Benedetti, Anna Maria Capelli, Palmina Cavallini, Paolo Cavanni, Silvia Davalli, Daniele Donati, Aldo Feriani, Sylvie Gehanne, Mahmoud Hamdan, Micaela Maffeis, Fabio Maria Sabbatini, Maria Elvira Tranquillini, Monica Valeria Angela Viziano.   

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.

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Year:  2004        PMID: 14987980     DOI: 10.1016/j.farmac.2003.12.005

Source DB:  PubMed          Journal:  Farmaco        ISSN: 0014-827X


  1 in total

1.  Synthesis of G-N2-(CH2)3-N2-G Trimethylene DNA interstrand cross-links.

Authors:  Francesca Gruppi; Tracy L Johnson Salyard; Carmelo J Rizzo
Journal:  Curr Protoc Nucleic Acid Chem       Date:  2014-03-26
  1 in total

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