Identification of a novel NR2B-selective NMDA receptor antagonist using a virtual screening approach.
نویسندگان
چکیده
We report the identification of a novel NR2B-selective NMDAR antagonist with an original scaffold, LSP10-0500. This compound was identified by a virtual high-throughput screening approach on the basis of a quantitative pharmacophore model of NR2B-specific NMDAR antagonists. A SAR study around LSP10-0500 is also described.
منابع مشابه
Synthesis of a carbon-14 analogue of N-(aryl-methyl)-3-phenyl-acryl amidine-[carboxy-14C] and its derivatives as NR2B-selective NMDA receptor antagonist
Four amidine NR2B-selective NMDA receptor antagonists, N-( 2-methoxy benzyl) -3-phenyl-acrylamidine, N-[diduterio(2-methoxyphenyl) methyl]-3-phenyl-acrylamidine, N-benzyl-3-phenyl-acryl amidine and N-[diduterio(phenyl)methyl]-3-phenyl-acrylamidine, all fourlabeled with carbon-14 in the 1-position, have been synthesized as part of 5-step sequence fromBa14CO3.
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ورودعنوان ژورنال:
- Bioorganic & medicinal chemistry letters
دوره 20 18 شماره
صفحات -
تاریخ انتشار 2010