| 摘要 |
Mammalian collagenase is inhibited by compounds of the formula <IMAGE> or salts thereof, wherein R is hydrogen, alkanoyl of 2 to 10 carbon atoms or arylcarbonyl; R1 is of 3 to 8 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, aryl or arylalkyl; <IMAGE> <IMAGE> <IMAGE> +TR <IMAGE> R4 is hydrogen, methyl, ethyl, or <IMAGE> R5 and R6 are each independently selected as -OCH3 or -OCH2CH3 or are combined as -OCH2 CH2O- or -O-(CH2)-O-; R7 and R8 are each independently selected as hydrogen, methyl or ethyl or are combined as -(CH2)4-, -(CH2)5- or -CH2CH2-O-CH2CH2-; R9 is hydrogen, methyl, ethyl <IMAGE> m is an integer from 0 to 7; p is an integer from 1 to 3; AAn is an amino acid chain of from one to three amino acids; n is 1 or 1, 2 or 1, 2, 3; when p is 1, AAn is AA1; when p is 2, AAn is AA1-AA2; when p is 3, AAn is AA1-AA2-AA3; AA1 is glycine or alanine; AA2 is glycine or alanine; AA3 is leucine, glutamine or isoleucine. A method of reducing the adverse effects of mammalian collagenase in a mammalian host in need thereof, which comprises administering to the mammal an effective amount of a compound having the above formula is within the scope of the invention. |
