Overall synthesis of GSK356278: quick delivery of a PDE4 inhibitor using a fit-for-purpose approach

…, D Castoldi, N Giubellina, A Lamonica…

Index: Guercio, Giuseppe; Castoldi, Damiano; Giubellina, Nicola; Lamonica, Alessandro; Ribecai, Arianna; Stabile, Paolo; Westerduin, Pieter; Dams, Riet; Nicoletti, Anna; Rossi, Sara; Bismara, Claudio; Provera, Stefano; Turco, Lucilla Organic Process Research and Development, 2010 , vol. 14, # 5 p. 1153 - 1161

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Citation Number: 4

Abstract

The family of phosphodiesterase (PDE) enzymes hydrolyse cyclic nucleotides, cAMP and cGMP, leading to their inactivation as intracellular second messengers. Inhibition of these enzymes leads to an elevation of levels of cyclic nucleotides in the cell and prolongs their action on downstream signaling pathways. PDE4, of which there are four subtypes, is widely expressed throughout the brain but is also abundant in the periphery in inflammatory and ...