Title : Structure-activity relationships of substituted 1-pyridyl-2-phenyl-1,2-ethanediones: potent, selective carboxylesterase inhibitors - Young_2010_J.Med.Chem_53_8709 |
Author(s) : Young BM , Hyatt JL , Bouck DC , Chen T , Hanumesh P , Price J , Boyd VA , Potter PM , Webb TR |
Ref : Journal of Medicinal Chemistry , 53 :8709 , 2010 |
Abstract :
Inhibition of intestinal carboxylesterases may allow modification of the pharmacokinetics/pharmacodynamic profile of existing drugs by altering half-life or toxicity. Since previously identified diarylethane-1,2-dione inhibitors are decidedly hydrophobic, a modified dione scaffold was designed and elaborated into a >300 member library, which was subsequently screened to establish the SAR for esterase inhibition. This allowed the identification of single digit nanomolar hiCE inhibitors that showed improvement in selectivity and measured solubility. |
PubMedSearch : Young_2010_J.Med.Chem_53_8709 |
PubMedID: 21105730 |
Young BM, Hyatt JL, Bouck DC, Chen T, Hanumesh P, Price J, Boyd VA, Potter PM, Webb TR (2010)
Structure-activity relationships of substituted 1-pyridyl-2-phenyl-1,2-ethanediones: potent, selective carboxylesterase inhibitors
Journal of Medicinal Chemistry
53 :8709
Young BM, Hyatt JL, Bouck DC, Chen T, Hanumesh P, Price J, Boyd VA, Potter PM, Webb TR (2010)
Journal of Medicinal Chemistry
53 :8709