Novel, highly potent adenosine deaminase inhibitors containing the pyrazolo [3, 4-d] pyrimidine ring system. Synthesis, structure-activity relationships, and molecular …

…, L Mugnaini, A Lavecchia, E Novellino…

Index: Da Settimo, Federico; Primofiore, Giampaolo; La Motta, Concettina; Taliani, Sabrina; Simorini, Francesca; Marini, Anna Maria; Mugnaini, Laura; Lavecchia, Antonio; Novellino, Ettore; Tuscano, Daniela; Martini, Claudia Journal of Medicinal Chemistry, 2005 , vol. 48, # 16 p. 5162 - 5174

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Citation Number: 46

Abstract

This study reports the synthesis of a number of 1-and 2-alkyl derivatives of the 4- aminopyrazolo [3, 4-d] pyrimidine (APP) nucleus and their evaluation as inhibitors of ADA from bovine spleen. The 2-substituted aminopyrazolopyrimidines proved to be potent inhibitors, most of them exhibiting K i values in the nanomolar/subnanomolar range. In this series the inhibitory activity is enhanced with the increase in length of the alkyl chain, ...