Synthesis of C-2 symmetric potential inhibitors of HIV-1 protease from D-mannitol

被引:4
作者
Niklasson, G
Kvarnstrom, I
Classon, B
Samuelsson, B
Nillroth, U
Danielson, H
Karlen, A
Hallberg, A
机构
[1] UNIV STOCKHOLM,ARRHENIUS LAB,DEPT ORGAN CHEM,S-10691 STOCKHOLM,SWEDEN
[2] LINKOPING UNIV,DEPT CHEM,S-58183 LINKOPING,SWEDEN
[3] UNIV UPPSALA,CTR BIOMED,DEPT BIOCHEM,S-75123 UPPSALA,SWEDEN
[4] UNIV UPPSALA,CTR BIOMED,DEPT ORGAN PHARMACEUT CHEM,S-75123 UPPSALA,SWEDEN
[5] ASTRA HASSLE AB,S-43183 MOLNDAL,SWEDEN
关键词
D O I
10.1080/07328309608005674
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
D-Mannitol was used as precursor for the synthesis of acyclic C-2 symmetric potential HIV-1 protease inhibitors. The 1- and 6-hydroxy groups of D-mannitol were substituted by -NHBoc, -NHValZ, -SAr, -SOAr and -SO2Ar and the 2- and 5-hydroxy groups were benzylated. In some products one of the central hydroxyl groups was either inverted or deoxygenated. Despite a close structural similarity to previously published inhibitors none of the products showed significant inhibitory activity against HIV-1 protease.
引用
收藏
页码:555 / 569
页数:15
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