Design of novel neurokinin 1 receptor antagonists based on conformationally constrained aromatic amino acids and discovery of a potent chimeric opioid agonist-neurokinin 1 receptor antagonist

A screening of conformationally constrained aromatic amino acids as base cores for the preparation of new NK1 receptor antagonists resulted in the discovery of three new NK1 receptor antagonists, 19 [Ac-Aba-Gly-NH-3′,5′-(CF(3))(2)-Bn], 20 [Ac-Aba-Gly-NMe-3′,5′-(CF(3))(2)-Bn] and 23 [Ac-Tic-NMe-3′,5′...

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Bibliographic Details
Main Authors: Ballet, Steven, Feytens, Debby, Buysse, Koen, Chung, Nga N., Lemieux, Carole, Tumati, Suneeta, Keresztes, Attila, Van Duppen, Joost, Lai, Josephine, Varga, Eva, Porreca, Frank, Schiller, Peter W., Broeck, Jozef Vanden, Tourwé, Dirk
Format: Artigo
Language:Inglês
Published: 2011
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Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC3096782/
https://ncbi.nlm.nih.gov/pubmed/21413804
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm1016285
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