Stepwise modulation of neurokinin-3 and neurokinin-2 receptor affinity and selectivity in quinoline tachykinin receptor antagonists

…, S Gagliardi, MA Luttmann, M Martinelli…

文献索引：Blaney; Raveglia; Artico; Cavagnera; Dartois; Farina; Grugni; Gagliardi; Luttmann; Martinelli; Nadler; Parini; Petrillo; Sarau; Scheideler; Hay; Giardina Journal of Medicinal Chemistry, 2001 , vol. 44, # 11 p. 1675 - 1689

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被引用次数: 47

摘要

A stepwise chemical modification from human neurokinin-3 receptor (hNK-3R)-selective antagonists to potent and combined hNK-3R and hNK-2R antagonists using the same 2- phenylquinoline template is described. Docking studies with 3-D models of the hNK-3 and hNK-2 receptors were used to drive the chemical design and speed up the identification of potent and combined antagonsits at both receptors.(S)-(+)-N-(1-Cyclohexylethyl)-3-[(4- ...