Studies on neurokinin antagonists. 2. Design and structure-activity relationships of novel tripeptide substance P antagonists, N. alpha.-[N. alpha.-(N. alpha.-acetyl-L- …

…, H Miyake, H Morimoto, M Murai, T Fujii…

文献索引：Hagiwara, Daijiro; Miyake, Hiroshi; Morimoto, Hiroshi; Murai, Masako; Fujii, Takashi; Matsuo, Masaaki Journal of Medicinal Chemistry, 1992 , vol. 35, # 17 p. 3184 - 3191

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被引用次数: 28

摘要

Continuing studies on the chemical modification of the previously reported novel tripeptide SP antagonist, Nu-[Nu-[Nu-(tert-butyloxycarbonyl) glutaminyl]-~-formyl-~-tryptophyl] phenylalanine benzyl ester [Boc-Gln-D-Trp-(CH0)-Phe-OBzl (l)], are described herein. We initially investigated the stability of 1 in guinea pig plasma and liver homogenate to elucidate the most labile part in the structure. It was consequently revealed that the benzyl ester part ...