Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists |
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| Authors: | Kulkarni Santosh S Nightingale Barbara Dersch Christina M Rothman Richard B Newman Amy Hauck |
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| Institution: | Medicinal Chemistry Section, National Institute on Drug Abuse, Intramural Research Program, NIH, DHHS, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA. |
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| Abstract: | A series of diaryl amides was designed and synthesized as novel nonethynyl mGluR5 antagonists. The systematic variation of the pharmacophoric groups led to the identification of a lead compound that demonstrated micromolar affinity for the mGluR5. Further optimization resulted in compounds with improved binding affinities and antagonist profiles, in vitro. |
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