Ito H, Tsutida Y
Jpn J Antibiot. 1983 Dec;36(12):3349-54.
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.
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。
