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ID: ALA1158608

Journal: Bioorg Med Chem Lett

Title: Hit-to-lead optimization of disubstituted oxadiazoles and tetrazoles as mGluR5 NAMs.

Authors: Wágner G, Wéber C, Nyéki O, Nógrádi K, Bielik A, Molnár L, Bobok A, Horváth A, Kiss B, Kolok S, Nagy J, Kurkó D, Gál K, Greiner I, Szombathelyi Z, Keseru GM, Domány G.

Abstract: Here we report the discovery and early SAR of a series of mGluR5 negative allosteric modulators (NAMs). Starting from a moderately active HTS hit we synthesized 3,5-disubstituted-oxadiazoles and tetrazoles as mGluR5 NAMs. Based on the analysis of ligand efficiency and lipophilic efficiency metrics we identified a promising lead candidate as a starting point for further optimization.

CiteXplore: 20483612

DOI: 10.1016/j.bmcl.2010.04.075