Structure–activity relationships of novel endomorphin-2 analogues with N–O turns induced by α-aminoxy acids

…, X Shao, M Gong, B Zhu, Y Cui, Y Gao, R Wang

Index: Wei, Jie; Shao, Xuan; Gong, Maozhen; Zhu, Beibei; Cui, Yuxin; Gao, Yanfeng; Wang, Rui Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 12 p. 2986 - 2989

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Citation Number: 14

Abstract

Endomorphin-2 (H-Tyr-Pro-Phe-Phe-NH2, EM-2) is a putative endogenous μ-opioid receptor ligand. To study the structure–activity relationship against its receptor, we introduced N–O turns into EM-2 and got the analogues with potent affinities for μ-opioid receptor. Our results indicated that N–O turn structures at the Pro2-aminoxy-Phe3 position of EM-2 analogues played important roles for their affinities. These novel analogues with N– ...