Exploration of secondary and tertiary pharmacophores in unsymmetrical N,N'-diaryl urea inhibitors of soluble epoxide hydrolase.
The impact of various secondary and tertiary pharmacophores on in vitro potency of soluble epoxide hydrolase (sEH) inhibitors based on the unsymmetrical urea scaffold 1 is discussed. N,N'-Diaryl urea inhibitors of soluble epoxide hydrolase exhibit subtle variations in inhibitory potency depending on the secondary pharmacophore but tolerate considerable structural variation in the second linker/tertiary pharmacophore fragment.
Anandan
Sampath-Kumar
SK
Arête Therapeutics, Inc., 7000 Shoreline Court, South San Francisco, CA 94080, USA. anandan30@yahoo.com
Gless
Richard D
RD
D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D004851:Epoxide Hydrolases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008956:Models, Chemical; D008958:Models, Molecular; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
D004791:Enzyme Inhibitors; D014508:Urea; D004851:Epoxide Hydrolases