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ID: ALA1208754
Journal: Bioorg Med Chem Lett
Title: Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists.
Authors: Galambos J, Wágner G, Nógrádi K, Bielik A, Molnár L, Bobok A, Horváth A, Kiss B, Kolok S, Nagy J, Kurkó D, Bakk ML, Vastag M, Sághy K, Gyertyán I, Gál K, Greiner I, Szombathelyi Z, Keseru GM, Domány G.
Abstract: Hit-to-lead optimization of a HTS hit led to new carbamoyloxime derivatives. After identification of an advanced hit (8d) the CYP enzyme inhibitory activity of this class of compounds was successfully eliminated. Systematic exploration of different parts of the advanced hit led us to some promising lead compounds with mGluR5 affinities comparable to that of MPEP.
CiteXplore: 20615697