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Bioorg Med Chem Lett. 2002 Nov 4;12(21):3219-22.

Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists.

Author information

1
GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA.

Abstract

The ultrashort-acting benzodiazepine (USA BZD) agonists reported previously have been structurally modified to improve aqueous solubility. Lactam-to-amidine modifications, replacement of the C5-haloaryl ring, and annulation of heterocycles are presented. These analogues retain BZD receptor potency and full agonism profiles.

PMID:
12372538
DOI:
10.1016/s0960-894x(02)00513-9
[Indexed for MEDLINE]

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