| 摘要 |
Compounds of formula (I), wherein A and A are independently the same or different group of formula (II) wherein: R' is H, CH3, C(CH3)2,-ORa, -N(Ra)2, -N(Ra)ORa or -DP; R is H or CH3; Ra is H, C1-C3 alkyl; D is a bond, alkylene, -C(=O)-, -S(O)- or S(O)2-; P is an optionally substituted, mono or bicyclic carbo- or hetereocycle; R'' is H, any of the sidechains found in the natural amino acids, carboxacetamide, or a group (CH2)nDP; M is a bond or -C(=O)N(R''')-; Q is absent, a bond, -CH(OH)- or CH2-; or R'' together with Q, M and R define an optionally substituted 5 or 6 membered carbo- or heterocyclic ring which is optionally fused with a further 5 or 6 membered carbo- or heterocyclic ring; with the proviso that R is -ORa, -, N(Ra)2, -N(Ra)ORa or -DP, if M is a bond and Q is absent; X is H, OH, OCH3, Y is H, OH, OCH3, but X and Y are not both H; Z' and Z'' are independently -(CH2)mP where P is as defined above; n and m are independently 0, 1 or 2; and pharmaceutically acceptable salts and prodrugs thereof have utility as aspartyl protease inhibitors of HIV. They can be prepared in a facile two step synthesis from novel 2,5-di-O-benzyl-L-mannaro-1,4:6,3-dilactone intermediates.
|
