| 摘要 |
Peptidyl compounds having an imidazole substituent of general formula (I), wherein R1 is a C1-6 alkyl, C2-6 alkenyl, (C1-6 alkyl) aryl, aryl, C1-6 alkylheteroaryl, heteroaryl or C1-6 alkyl-AR9 group where A is O, NR9 or S(O)m where m = 0-2, and R9 is H, C1-4 alkyl, aryl, heteroaryl, (C1-4 alkyl)aryl or (C1-4 alkyl)heteroaryl; if A=NR9 the groups R9 may be the same or different; R2 is hydrogen or a C1-6 alkyl group; R3 is a ¢Alk!nR6 group where Alk is a C16 alkyl or C2-6 alkenyl group and n is zero or 1; X is NR9, O or S; Y is N or CR4; R4 and R5 are the same or different and are R9, COR13, C1-3 alkyl-R13 or C1-3 alkyl-COR13; R7 is hydrogen or R10CO where R10 is C1-4 alkyl, C1-4 alkylaryl, C1-4 alkylheteroaryl, cyclo(C3-6)alkyl, C1-4 alkyl-cyclo(C3- 6)alkyl, C2-6 alkenyl, C2-6 alkenylaryl, aryl or heteroaryl; R8 is aryl (optionally substituted with R11), heteroaryl (optionally substituted with R11), C1-4 alkyl (optionally substituted with R11), etc., have therapeutic utility via their inhibitory effect on metalloproteinases and tumour necrosis factor.
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