| 摘要 |
A compound of formula II:
wherein:
R 2' and R 2" are each independently hydrogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, aryl, heterocyclic, heteroaromatic or a prodrug moiety;
R 10 , R 11 and R 12 are each independently hydrogen, alkyl, aryl, benzyl, arylalkyl, or a pro-drug moiety;
R 3' is hydroxyl, hydrogen, or a pro-drug moiety;
R 4 is NR 4c R 4d ;
R 4c and R 4d are each independently hydrogen, sulfonyl, arylcarbonyl, arylaminocarbonyl, aryloxycarbonyl, alkylcarbonyl, alkylaminocarbonyl, alkyloxycarbonyl, acyl, alkyl, alkenyl, alkynyl, or aryl;
R 5 and R 5' are each independently hydroxyl, hydrogen, thiol, alkanoyl, aroyl, alkaroyl, aryl, heteroaromatic, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, alkyl carbonyloxy, or aryl carbonyloxy;
R 6 and R 6' are each independently hydrogen, methylene, absent, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
R 7 is hydrogen, hydroxyl, halogen, thiol, nitro, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, arylalkyl, amino, arylalkenyl, arylalkynyl, acyl, aminoalkyl, heterocyclic, thionitroso, or-(CH 2 ) 0-3 (NR 7c ) 0-1 CC(=W')WR 7a ;
R 8 is hydrogen, hydroxyl, halogen, thiol, nitro, alkyl, alkenyl, alkynyl, aryl, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, amino, arylalkenyl, arylalkynyl, alkoxy, acyl, aminoalkyl, heterocyclic, thionitroso, or-(CH 2 ) 0-3 (NR 8c ) 0-1 C(=E')ER 8a ;
R 9 is hydrogen, hydroxyl, halogen, thiol, nitro, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, arylalkyl, amino, arylalkenyl, arylalkynyl, acyl, aminoalkyl, heterocyclic, thionitroso, or-(CH 2 ) 0-3 (NR 9c ) 0-1 C(=Z')ZR 9a ;
R 7a , R 7b , R 7c , R 7d , R 7e , R 7f , R 8a , R 8b , R 8c , R 8d , R 8e , R 8f , R 9a , R 9b , R 9c , R 9d , R 9e , and R 9f are each independently hydrogen, acyl, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, aryl, heterocyclic, heteroaromatic or a prodrug moiety;
R 13 is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, aryl, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
E is CR 8d R 8e , S, NR 8b or O;
E' is O, NR 8f , or S;
W is CR 7d R 7e , S, NR 7b or O;
W' is O, NR 7f , or S;
X is CHC(R 13 Y'Y), C=CR 13 Y, CR 6' R 6 , S, NR 6 , or O;
Y' and Y are each independently hydrogen, halogen, hydroxyl, cyano, sulfhydryl, amino, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
Z is CR 9d R 9e , S, NR 9b or 0;
Z' is O, S, or NR 9f , or a pharmaceutically acceptable salt, ester or enantiomer thereof.
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