Design and synthesis of side-chain conformationally restricted phenylalanines and their use for structure-activity studies on tachykinin NK-1 receptor

H Josien, S Lavielle, A Brunissen…

文献索引：Josien, Hubert; Lavielle, Solange; Brunissen, Alie; Saffroy, Monique; Torrens, Yvette; et al. Journal of Medicinal Chemistry, 1994 , vol. 37, # 11 p. 1586 - 1601

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被引用次数: 81

摘要

Constrained analogues of phenylalanine have been conceptually designed for analyzing the binding pockets of Phe7 (S7) and Phea (Sa), two aromatic residues important for the pharmacological properties of SP, ie, L-tetrahydroisoquinoleic acid, L-diphenylalanine, L-9- fluorenylglycine (Flg), 24ndanylglycine, the diastereomers of Ll-indanylglycine (Ing) and Ll- benz [flindanylglycine (Bfi), and the 2 and E isomers of dehydrophenylalanine (AZPhe, ...