Medicinal Chemistry

Design, synthesis and anti-itch activity evaluation of aromatic amino acid derivatives as gastrin-releasing peptide receptor antagonists

RS Yao, TT Li, J Xu, LE Jiang, BF Ruan

Index: Yao, Ri-Sheng; Li, Ting-Ting; Xu, Jun; Jiang, Lai-En; Ruan, Ban-Feng Medicinal Chemistry, 2012 , vol. 8, # 5 p. 865 - 873

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Citation Number: 4

Abstract

Eight aromatic amino acid derivatives (9a-9h) as gastrin-releasing peptide receptor (GRPR) antagonists were designed and synthesized. For the design, the tertiary structure of GRPR was predicted by blast searching in the premise of 1u19 protein as the template. Eight target compounds were docked into the binding pocket to investigate their possible binding interactions. Their anti-itch activities were tested by intrathecal injection using Kunming ...