Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists

…, L Molnár, A Bobok, A Horváth, B Kiss, S Kolok…

文献索引：Galambos, Janos; Wagner, Gabor; Nogradi, Katalin; Bielik, Attila; Molnar, Laszlo; Bobok, Amrita; Horvath, Attila; Kiss, Bela; Kolok, Sandor; Nagy, Jozsef; Kurko, Dalma; Bakk, Monika L.; Vastag, Monika; Saghy, Katalin; Gyertyan, Istvan; Gal, Krisztina; Greiner, Istvan; Szombathelyi, Zsolt; Keser, Gyoergy M.; Domany, Gyoergy Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 15 p. 4371 - 4375

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被引用次数: 12

摘要

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.