DIFUNCTIONAL ENOLS OF N-PROTECTED AMINO-ACIDS AS LOW-MOLECULAR-WEIGHT AND NOVEL INHIBITORS OF HIV-1 PROTEASE

被引：14

作者：

VAILLANCOURT, M

VANASSE, B

COHEN, E

SAUVE, G

机构：

[1] UNIV QUEBEC, INST ARMAND FRAPPIER, 531 BOUL PRAIRIES, LAVAL H7N 4Z3, QUEBEC, CANADA

[2] UNIV MONTREAL, DEPT MICROBIOL & IMMUNOL, MONTREAL H3C 3J7, QUEBEC, CANADA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(00)80308-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis of difunctional enols of simple amino acids and their novel inhibitory activity against human immunodeficiency virus type 1 protease (HIV-PR) are described. By modifying the substituents on these enols, we were able to achieve mid-nanomolar range in activity against HIV-1 protease which is, to our knowledge, the best reported activity for molecules that do not contain at least one peptide linkage.

引用

收藏

页码：1169 / 1174

页数：6

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