Trisubstituted Imidazoles as Positive Modulators of Metabotropic Glutamate Receptor Subtype 5
نویسندگان
چکیده
منابع مشابه
Identification of glutathione conjugates of acetylene-containing positive allosteric modulators of metabotropic glutamate receptor subtype 5.
A recent medicinal chemistry campaign to identify positive allosteric modulators (PAMs) of metabotropic glutamate receptor subtype 5 (mGluR5) led to the discovery of potent compounds featuring an oxazolidinone structural core flanked by biaryl acetylene and haloaryl moieties. However, biotransformation studies of some of these mGluR5 PAMs demonstrated the formation of glutathione (GSH) conjugat...
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Positive allosteric modulators (PAMs) of metabotropic glutamate receptor 5 (mGlu5) represent a promising therapeutic strategy for the treatment of schizophrenia. Starting from an acetylene-based lead from high throughput screening, an evolved bicyclic dihydronaphthyridinone was identified. We describe further refinements leading to both dihydronaphthyridinone and tetrahydronaphthyridine mGlu5 P...
متن کاملIdentification of Glutathione Conjugates of Acetylene- Containing Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype
XIAOLIANG ZHUO, XIAOHUA STELLA HUANG, ANDREW P. DEGNAN, LAWRENCE B. SNYDER, FUKANG YANG, HONG HUANG, YUE-ZHONG SHU, BENJAMIN M. JOHNSON Department of Biotransformation (X.Z., B.M.J.), Discovery Analytical Sciences (X.S.H.), Neuroscience Chemistry (A.P.D., L.B.S., F.Y., H.H.), Bristol-Myers Squibb Co., 5 Research Parkway, Wallingford, CT 06492 Department of Biotransformation (Y.-Z.S.), Bristol-M...
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We have identified a family of highly selective allosteric modulators of the group I metabotropic glutamate receptor subtype 5 (mGluR5). This family of closely related analogs exerts a spectrum of effects, ranging from positive to negative allosteric modulation, and includes compounds that do not themselves modulate mGluR5 agonist activity but rather prevent other family members from exerting t...
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Activation of metabotropic glutamate receptor subtype 4 has been shown to be efficacious in rodent models of Parkinson's disease. Artificial neural networks were trained based on a recently reported high throughput screen which identified 434 positive allosteric modulators of metabotropic glutamate receptor subtype 4 out of a set of approximately 155,000 compounds. A jury system containing thre...
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ژورنال
عنوان ژورنال: ACS Medicinal Chemistry Letters
سال: 2013
ISSN: 1948-5875,1948-5875
DOI: 10.1021/ml4002776