Document Report Card

Basic Information

ID: ALA1932998

Journal: Bioorg Med Chem

Title: Design, synthesis and evaluation of polar head group containing 2-keto-oxazole inhibitors of FAAH.

Authors: Rusch M, Zahov S, Vetter IR, Lehr M, Hedberg C.

Abstract: 2-α-Keto oxazoles containing polar head groups in their C5-side chains were designed as fatty acid amide hydrolase (FAAH) inhibitors. Variation in the spacer length resulted in submicromolar α-keto-oxazole FAAH inhibitor (IC(50)=436 nM) presenting electrostatic stabilizing interactions between its polar head group contained in the C5-side chain and the hydrophilic pocket of the enzyme.

CiteXplore: 22196515

DOI: 10.1016/j.bmc.2011.11.027