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3-[Substituted]-5-(5-pyridin-2-yl-2 H-tetrazol-2-yl)benzonitriles: Identification of highly potent and selective metabotropic glutamate subtype 5 receptor antagonists
Structure–activity relationship studies on the phenyl ring of 3-(5-pyridin-2-yl-2 H-tetrazol-2-yl)benzonitrile 2 led to the discovery that small, non-hydrogen bond donor substituents at the 3-position led to a substantial increase in in vitro potency. In particular, 3-fluoro-5-(5-pyridin-2-yl-2 H-te...
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Published in: | Bioorganic & medicinal chemistry letters 2005-11, Vol.15 (22), p.5061-5064 |
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Main Authors: | , , , , , , , , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites Items that cite this one |
Online Access: | Get full text |
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Summary: | Structure–activity relationship studies on the phenyl ring of 3-(5-pyridin-2-yl-2
H-tetrazol-2-yl)benzonitrile
2 led to the discovery that small, non-hydrogen bond donor substituents at the 3-position led to a substantial increase in in vitro potency. In particular, 3-fluoro-5-(5-pyridin-2-yl-2
H-tetrazol-2-yl)benzonitrile (
7) is a highly potent and selective mGlu5 receptor antagonist with good rat pharmacokinetics, brain penetration, and in vivo receptor occupancy.
Structure–activity relationship studies on the phenyl ring of 3-(5-pyridin-2-yl-2
H-tetrazol-2-yl)benzonitrile
2 led to the discovery that small, non-hydrogen bond donor substituents at the 3-position led to a substantial increase in in vitro potency. In particular, 3-fluoro-5-(5-pyridin-2-yl-2
H-tetrazol-2-yl)benzonitrile (
7) is a highly potent and selective mGlu5 receptor antagonist with good rat pharmacokinetics, brain penetration, and in vivo receptor occupancy. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2005.07.062 |