�ber die Geschwindigkeit der Aminolyse von verschiedenen neuen, aktivierten, N-gesch�tzten ?-Aminos�ure-phenylestern, insbesondere 2,4,5-Trichlorphenylestern
作者:J. Pless、R. A. Boissonnas
DOI:10.1002/hlca.19630460516
日期:——
A comparison of the ate of aminolysis of many substituted phenyl esters of N-protected α-amino-acids shows that the 2,4,5-trichlorophenyl esters are promising new active derivatives for the synthesis of peptides.
The N alpha-(2-chloroethyl)-N-nitrosocarbamoyl derivatives of H-Pro-Lys(X)-Pro-Val-NH2 (X: tert-butyloxycarbonyl, formyl, (2-chloroethyl)nitrosocarbamoyl) were synthesized. It was found that the bis-substitution of the urea N3 in these derivatives does not decrease the antitumoractivity influenced mainly by the nature of the carrier molecule as a whole.
Synthesis of the decapeptide, histidylphenylalanylarginyltryptophylglycylserylprolylprolyl-lysylaspartic acid (I) corresponding to the C-terminal portion of β-melanocyte-stimulating hormones (β-MSH) from pig, sheep, beef, monkey and human was described. I was obtained by deformylation of histidylphenylalanylarginyltryptophylglycylserylprolylprolyl -Nε- formyllysylaspartic acid (II) with aqueous hydrazine. The MSH activity of I and II was examined in vitro. It was found that I and II exhibited the activity, 2.4×106 and 1.0×106 MSH U/g. respectively.
描述了与猪、绵羊、牛肉、猴和人的 β-黑素细胞刺激素(β-MSH)C-末端部分相对应的十肽组氨酰苯丙氨酰亚精氨酰禽肽甘氨酰亚精氨酰丙氨酰-赖氨酰天冬氨酸(I)的合成。组氨酰苯丙氨酰精氨酰色氨酰甘氨酰丝氨酰丙氨酰-Nε-甲酰丙氨酰天冬氨酸(II)经肼水溶液脱氨化得到 I。体外检测了 I 和 II 的 MSH 活性。结果发现,I 和 II 的活性分别为 2.4×106 和 1.0×106 MSH U/g.
Scoffone,E. et al., Gazzetta Chimica Italiana, 1964, vol. 94, p. 743 - 759
作者:Scoffone,E. et al.
DOI:——
日期:——
Studies on Polypeptides. XVI. The Preparation of N<sup>ε</sup>-Formyl-L-lysine and its Application to the Synthesis of Peptides<sup>1,2</sup>
作者:Klaus Hofmann、Erhard Stutz、Gertrude Spühler、Haruaki Yajima、Eleanore T. Schwartz