Title: Discovery of 7-N-Piperazinylthiazolo[5,4-d]pyrimidine Analogues as a Novel Class of Immunosuppressive Agents with in Vivo Biological Activity
Authors: 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 # ×
Issue Date: Jan-2011
Publisher: ACS Publications
Series Title: Journal of Medicinal Chemistry vol:54 issue:2 pages:655-668
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 potent congeners displayed IC50 values of less than 50 nM in this MLR assay and hence are equipotent to cyclosporin A, a clinically used immunosuppressive drug. One representative of this series was further evaluated in a preclinical animal model of organ transplantation and showed excellent in vivo efficacy. It validates these compounds as new promising immunosuppressive drugs.
ISSN: 0022-2623
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Medicinal Chemistry (Rega Institute)
Department of Experimental Medicine (-)
Laboratory of Experimental Transplantation
Interface Valorization Platform (IVAP) (-)
Department of Pharmaceutical & Pharmacological Sciences - miscellaneous
× corresponding author
# (joint) last author

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