917812-43-2Relevant academic research and scientific papers
Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG)
Tsagris, Denise J.,Birchall, Kristian,Bouloc, Nathalie,Large, Jonathan M.,Merritt, Andy,Smiljanic-Hurley, Ela,Wheldon, Mary,Ansell, Keith H.,Kettleborough, Catherine,Whalley, David,Stewart, Lindsay B.,Bowyer, Paul W.,Baker, David A.,Osborne, Simon A.
, p. 3168 - 3173 (2018/09/11)
A series of trisubstituted thiazoles have been identified as potent inhibitors of Plasmodium falciparum (Pf) cGMP-dependent protein kinase (PfPKG) through template hopping from known Eimeria PKG (EtPKG) inhibitors. The thiazole series has yielded compounds with improved potency, kinase selectivity and good in vitro ADME properties. These compounds could be useful tools in the development of new anti-malarial drugs in the fight against drug resistant malaria.
NEW SUBSTITUTED 1,3-THIAZOLE DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF HAVING IMMUNOSUPPRESSION AND INFLAMMATION INHIBITORY ACITIVITY, INTERMEDIATE COMPOUNDS OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, A PROCESS FOR THE PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Page/Page column 221, (2010/11/25)
Disclosed relates to new substituted 1,3-thiazole derivatives or pharmaceutically acceptable salts thereof having immunosuppresion and inflammation inhibitory activity, intermediate compounds or pharmaceutically acceptable salts thereof, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The compound of the present invention having excellent TNF-α inhibitory activity and inflammation inhibitory activity can be effectively used in the prevention and treatment of TNF-α related diseases.
