| 摘要 |
Compounds which inhibit Candida acid protease are disclosed which have the formula: <IMAGE> wherein R1 is loweralkyl, loweralkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, arylalkyl or (heterocyclic)alkyl; R2 is loweralkyl, cycloalkylalkyl or arylalkyl; R3 is -OH or -NH2; R4 is (a) -CH(OH)-R5 wherein R5 is loweralkyl, cycloalkyl or cycloalkylalkyl or (b) -CH2CH(R6)C(O)NHR7 wherein R6 is loweralkyl and R7 is loweralkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, hydroxyalkyl, alkoxyalkyl, thioalkoxyalkyl, carboxyalkyl, alkoxycarbonylalkyl, cyanoalkyl or (heterocyclic)alkyl; and A is <IMAGE> (a) wherein R8 is arylalkyl, B is -C(O) or -S(O)2- and R9 is aryl, arylalkyl, heterocyclic or (heterocyclic)alkyl; or <IMAGE> (b) wherein R10 is arylalkyl and R11 is (a) -C(O)R12 wherein R12 is alkoxy, arylalkoxy, aryl, arylalkyl, heterocyclic or (heterocyclic)alkyl or (b) -S(O)2-R13 wherein R13 is aryl, arylalkyl, heterocyclic or (heterocyclic)alkyl; or a pharmaceutically acceptable salt, ester or prodrug thereof.
|
