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Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists |
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| Authors: | János Galambos Gábor Wágner Katalin Nógrádi Attila Bielik László Molnár Amrita Bobok Attila Horváth Béla Kiss Sándor Kolok József Nagy Dalma Kurkó Mónika L Bakk Mónika Vastag Katalin Sághy István Gyertyán Krisztina Gál István Greiner Zsolt Szombathelyi György M Keserű György Domány |
| Institution: | Gedeon Richter Plc, Budapest 10, PO Box 27, H-1475, Hungary |
| 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. |
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