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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

2004; Elsevier BV; Volume: 59; Issue: 3 Linguagem: Inglês

10.1016/j.farmac.2003.12.005

1879-0569

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

Ion channel regulation and function

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.