1355478-10-2Relevant academic research and scientific papers
Synthesis and SAR study of imidazoquinolines as a novel structural class of microsomal prostaglandin E2 synthase-1 inhibitors
Shiro, Tomoya,Takahashi, Hirotada,Kakiguchi, Keisuke,Inoue, Yoshifumi,Masuda, Keiki,Nagata, Hidetaka,Tobe, Masanori
scheme or table, p. 285 - 288 (2012/02/16)
The imidazoquinoline derivative 1 was found as a novel mPGES-1 inhibitor. Optimization of 1 led to the identification of the 2-chlorophenyl group at the C(2)-position and the quinolone structure at the C(4)-position. Compound 33, the most potent synthesized compound, showed excellent mPGES-1 inhibition (IC 50 = 9.1 nM) with high selectivity (>1000-fold) over both COX-1 and COX-2.
