Mammalian collagenase is inhibited by compounds of the formula ##STR1## or salts thereof, wherein R is hydrogen, alkanoyl of 2 to 10 carbon atoms or arylcarbonyl; R.sub.1 is of 3 to 8 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, aryl or arylalkyl; ##STR2## R.sub.4 is hydrogen, methyl, ethyl, or ##STR3## R.sub.5 and R.sub.6 are each independently selected as --OCH.sub.3 or --OCH.sub.2 CH.sub.3 or are combined as --OCH.sub.2 CH.sub.2 O-- or --O--(CH.sub.2)--O--; R.sub.7 and R.sub.8 are each independently selected as hydrogen, methyl or ethyl or are combined as --(CH.sub.2).sub.4 --, --(CH.sub.2).sub.5 -- or --CH.sub.2 CH.sub.2 --O--CH.sub.2 CH.sub.2 --; R.sub.9 is hydrogen, methyl, ethyl ##STR4## m is an integer from 0 to 7; p is an integer from 1 to 3; AA.sub.n 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, AA.sub.n is AA.sub.1 ; when p is 2, AA.sub.n is AA.sub.1 --AA.sub.2 ; when p is 3, AA.sub.n is AA.sub.1 --AA.sub.2 --AA.sub.3 ; AA.sub.1 is glycine or alanine; AA.sub.2 is glycine or alanine; AA.sub.3 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.
Inventor(s):
Sundeen; Joseph E. (Yardley, PA), Dejneka; Tamara (Skillman, NJ)
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