期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 19, 期 20, 页码 6135-6142出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.08.027
关键词
Analgesic; Bivalent ligands; mu-Opioids; NK1 antagonist; Fentanyl
资金
- U.S. Public National Institute of Health [DA 13449, DA 06284, DA 06789]
- Division Of Chemistry
- Direct For Mathematical & Physical Scien [0741837, 840336] Funding Source: National Science Foundation
Newly designed bivalent ligands-opioid agonist/NK1-antagonists have been synthesized. The synthesis of new starting materials-carboxy-derivatives of Fentanyl (1a-1c) was developed. These products have been transformed to 'isoimidium perchlorates' (2a-c). The new isoimidium perchlorates have been successfully implemented in nucleophilic addition reactions, with L-tryptophan 3,5-bis(trifluoromethyl)benzyl ester to give the target compounds-amides (3a-c). Perchlorates (2a-c) successfully undergo reactions with other nucleophiles such as alcohols, amines or hydrazines. The obtained compound 3b exhibited mu-opioid agonist activity and NK1-antagonist activity and may serve as a useful lead compound for the further design of a new series of opioid agonist/NK1-antagonist compounds. Published by Elsevier Ltd.
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