Discovery of 7-N-piperazinylthiazolo [5, 4-d] pyrimidine analogues as a novel class of immunosuppressive agents with in vivo biological activity

…, LJ Gao, B Vanderhoydonck, M Froeyen…

Index: Jang, Mi-Yeon; Lin, Yuan; De Jonghe, Steven; Gao, Ling-Jie; Vanderhoydonck, Bart; Froeyen, Mathy; Rozenski, Jef; Herman, Jean; Louat, Thierry; Van Belle, Kristien; Waer, Mark; Herdewijn, Piet Journal of Medicinal Chemistry, 2011 , vol. 54, # 2 p. 655 - 668

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Citation Number: 27

Abstract

Herein we describe the synthesis and in vitro and in vivo activity of thiazolo [5, 4-d] pyrimidines as a novel class of immunosuppressive agents, useful for preventing graft rejection after organ transplantation. This research resulted in the discovery of a series of compounds with potent activity in the mixed lymphocyte reaction (MLR) assay, which is well- known as the in vitro model for in vivo rejection after organ transplantation. The most ...