Publications (2)2.65 Total impact
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Article: Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
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ABSTRACT: P2X purinoceptors are ligand-gated ion channels whose endogenous ligand is ATP. Both the P2X(3) and P2X(2/3) receptor subtypes have been shown to play an important role in the regulation of sensory function and dual P2X(3)/P2X(2/3) antagonists offer significant potential for the treatment of pain. A high-throughput screen of the Roche compound collection resulted in the identification of a novel series of diaminopyrimidines; subsequent optimization resulted in the discovery of RO-4, a potent, selective and drug-like dual P2X(3)/P2X(2/3) antagonist.Bioorganic & medicinal chemistry letters 03/2009; 19(6):1628-31. · 2.65 Impact Factor -
Article: Application of the “trimethyl lock”1 to Ganciclovir, a pro-prodrug with increased oral bioavailability
Bioorganic & Medicinal Chemistry Letters. 6(14):1653-1656.