| Literature DB >> 12372537 |
Jeffrey A Stafford1, Gregory J Pacofsky, Richard F Cox, Jill R Cowan, George F Dorsey, Stephen S Gonzales, David K Jung, George W Koszalka, Maggie S McIntyre, Jeffrey H Tidwell, Robert P Wiard, Paul L Feldman.
Abstract
The synthesis and evaluation of novel ultrashort-acting benzodiazepine (USA BZD) agonists is described. A BZD scaffold was modified by incorporation of amino acids and derivatives. The propionate side chain of glutamic acid tethers an enzymatically labile functionality where the metabolite carboxylic acid displays markedly reduced BZD receptor affinity. The USA BZDs were characterized by full agonism profiles. Copyright2000 Elsevier Science Ltd.Entities:
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Year: 2002 PMID： 12372537 DOI： 10.1016/s0960-894x(02)00512-7
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823