HIV蛋白酶抑制剂的设计与合成。HIV蛋白酶抑制剂L-682,679羧基末端的变体。
Design and synthesis of HIV protease inhibitors. Variations of the carboxy terminus of the HIV protease inhibitor L-682,679.
作者信息
deSolms S J, Giuliani E A, Guare J P, Vacca J P, Sanders W M, Graham S L, Wiggins J M, Darke P L, Sigal I S, Zugay J A
机构信息
Merck Sharp & Dohme Research Laboratories, West Point, Pennsylvania 19486.
出版信息
J Med Chem. 1991 Sep;34(9):2852-7. doi: 10.1021/jm00113a025.
A series of tetrapeptide analogues of 1 (L-682,679), in which the carboxy terminus has been shortened and modified, was prepared and their inhibitory activity measured against the HIV protease in a peptide cleavage assay. Selected examples were tested as inhibitors of virus spread in cell culture. Compound 12 was a 10-fold more potent enzyme inhibitor than 1 in vitro and 30-fold more potent in inhibiting the viral spread in cells.
制备了一系列1（L-682,679）的四肽类似物，其中羧基末端已被缩短和修饰，并在肽裂解试验中测定了它们对HIV蛋白酶的抑制活性。选择的实例作为细胞培养中病毒传播的抑制剂进行了测试。化合物12在体外是比1强10倍的酶抑制剂，在抑制细胞中病毒传播方面强30倍。
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