Ontology highlight
ABSTRACT:
SUBMITTER: Blocher R
PROVIDER: S-EPMC5933862 | biostudies-literature | 2018 Apr
REPOSITORIES: biostudies-literature
Blöcher René R Wagner Karen M KM Gopireddy Raghavender R RR Harris Todd R TR Wu Hao H Barnych Bogdan B Hwang Sung Hee SH Xiang Yang K YK Proschak Ewgenij E Morisseau Christophe C Hammock Bruce D BD
Journal of medicinal chemistry 20180410 8
Inspired by previously discovered enhanced analgesic efficacy between soluble epoxide hydrolase (sEH) and phosphodiesterase 4 (PDE4) inhibitors, we designed, synthesized and characterized 21 novel sEH/PDE4 dual inhibitors. The best of these displayed good efficacy in in vitro assays. Further pharmacokinetic studies of a subset of four selected compounds led to the identification of a bioavailable dual inhibitor N-(4-methoxy-2-(trifluoromethyl)benzyl)-1-propionylpiperidine-4-carboxamide (MPPA). I ...[more]