Back to Search
Start Over
Synthesis and SAR study of imidazoquinolines as a novel structural class of microsomal prostaglandin E2 synthase-1 inhibitors
- Source :
-
Bioorganic & Medicinal Chemistry Letters . Jan2012, Vol. 22 Issue 1, p285-288. 4p. - Publication Year :
- 2012
-
Abstract
- Abstract: 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 (IC50 =9.1nM) with high selectivity (>1000-fold) over both COX-1 and COX-2. [Copyright &y& Elsevier]
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 22
- Issue :
- 1
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 70156994
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.11.015