Ontology highlight
ABSTRACT:
SUBMITTER: Ballet S
PROVIDER: S-EPMC3096782 | biostudies-literature | 2011 Apr
REPOSITORIES: biostudies-literature
Ballet Steven S Feytens Debby D Buysse Koen K Chung Nga N NN Lemieux Carole C Tumati Suneeta S Keresztes Attila A Van Duppen Joost J Lai Josephine J Varga Eva E Porreca Frank F Schiller Peter W PW Vanden Broeck Jozef J Tourwé Dirk D
Journal of medicinal chemistry 20110317 7
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'-(CF(3))(2)-Bn], which were able to counteract the agonist effect of substance P, the endogenous ligand of NK1R. The most active NK1 antagonist of the series, 20 [Ac-Aba-Gly-NMe-3',5'-(CF(3))(2)-Bn], ...[more]