| abstract |
Peptidyl compounds having an imidazole substituent of general formula (I), wherein R<1> is a C1-6 alkyl, C2-6 alkenyl, (C1-6 alkyl) aryl, aryl, C1-6 alkylheteroaryl, heteroaryl or C1-6 alkyl-AR<9> group where A is O, NR<9> or S(O)m where m = 0-2, and R<9> is H, C1-4 alkyl, aryl, heteroaryl, (C1-4 alkyl)aryl or (C1-4 alkyl)heteroaryl; if A=NR<9> the groups R<9> may be the same or different; R<2> is hydrogen or a C1-6 alkyl group; R<3> is a [Alk]nR<6> group where Alk is a C1-6 alkyl or C2-6 alkenyl group and n is zero or 1; X is NR<9>, O or S; Y is N or CR<4>; R<4> and R<5> are the same or different and are R<9>, COR<13>, C1-3 alkyl-R<13> or C1-3 alkyl-COR<13>; R<7> is hydrogen or R<10>CO where R<10> 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; R<8> is aryl (optionally substituted with R<11>), heteroaryl (optionally substituted with R<11>), C1-4 alkyl (optionally substituted with R<11>), etc., have therapeutic utility via their inhibitory effect on metalloproteinases and tumour necrosis factor. |