Structure-activity relationship studies and pharmacological evaluation of 4-phenylthiazoles as dual soluble epoxide hydrolase/fatty acid amide hydrolase inhibitors.

ABSTRACT: Forty-two 4-phenylthiazole analogs, organized in two libraries 4a-u and 6a-u, were prepared and biologically evaluated in human fatty acid amide hydrolase (FAAH), and human, rat and mouse soluble epoxide hydrolase (sEH) inhibition assays. This structure-activity relationship (SAR) study explores the impact of electronic and steric changes on the molecule's potency and binding affinity to better understand the structural features important for dual sEH/FAAH inhibition which will guide the development of novel treatments for pain and inflammation. Our SAR revealed that electron-donating groups on the aromatic ring of the 4-phenylthiazole moiety are particularly well tolerated by both enzymes when placed at the ortho, meta and para positions; however, the overall 3D shape of the molecule is v

SUBMITTER: Yuan C 

PROVIDER: S-EPMC11910963 | biostudies-literature | 2025 Apr

REPOSITORIES: biostudies-literature