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…

Index: 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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Citation Number: 81

Abstract

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, ...