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[抗菌肽(XX)。含碱性氨基酸的α-酰基四肽的合成及抗菌活性(IX)]

[Antibacterial peptides (XX). Synthesis and antibacterial activity of alpha-acyltetrapeptides containing basic amino acids (IX)].

作者信息

Ito H, Tsutida Y

出版信息

Jpn J Antibiot. 1983 Dec;36(12):3349-54.

PMID:6674547
Abstract

In order to compare the antibacterial activity with Acyl-Lys-Lys(Thr)-Glu-OH (I), already reported, 3 kinds of Acyl-Lys-Lys(Glu)-Thr-OH (9a - c) and corresponding tetrapeptide (10), which were exchanged Thr for Glu on I, were synthesized by dicyclohexylcarbodiimide method. It was proved the (+)-6-methyloctanoyl-Lys-Lys(Glu)-Thr-OH (9a) shows antibacterial activity against 5 kinds of Gram-negative bacteria and against 2 kinds of Gram-positive bacteria, but that the others (9b), (9c), only have the weak one, and that tetrapeptide has against Gram-positive bacteria; and that those compounds have almost the same one as Acyl-Lys-Lys(Thr)-Glu-OH (I) has.

摘要

为了与已报道的酰基 - 赖氨酸 - 赖氨酸(苏氨酸) - 谷氨酸 - 羟基(I)的抗菌活性进行比较,通过二环己基碳二亚胺法合成了3种酰基 - 赖氨酸 - 赖氨酸(谷氨酸) - 苏氨酸 - 羟基(9a - c)以及在I中将苏氨酸换成谷氨酸的相应四肽(10)。结果证明,(+) - 6 - 甲基辛酰基 - 赖氨酸 - 赖氨酸(谷氨酸) - 苏氨酸 - 羟基(9a)对5种革兰氏阴性菌和2种革兰氏阳性菌具有抗菌活性,但其他化合物(9b)、(9c)只有微弱的抗菌活性,且四肽对革兰氏阳性菌有抗菌活性;并且这些化合物的抗菌活性与酰基 - 赖氨酸 - 赖氨酸(苏氨酸) - 谷氨酸 - 羟基(I)几乎相同。

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