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US5686422A Synthetic inhibitors of mammalian collagenase 失效
哺乳动物胶原酶的合成抑制剂

Synthetic inhibitors of mammalian collagenase
摘要:
The present invention relates to compounds of the formula: R.sub.1 SCH(R.sub.2)CH(R.sub.3)CO-AA.sub.1 �AA.sub.2 !.sub.m �AA.sub.3 !.sub.n --X or HSCH.sub.2 �CH.sub.2 CH(CH.sub.3).sub.2 !CO--Nal--NH.sub.2 wherein Nal is L-3-(2-naphthyl)alanine; m is the integer 0 or 1; n is an integer from 0-2; AA.sub.1 is a non-polar hydrophobic aromatic amino acid; AA.sub.2 is alanine, glycine, leucine, isoleucine or phenylalanine; AA.sub.3 is one of the twenty naturally occurring amino acids, preferably glutamine or arginine; R.sub.1 is hydrogen, alkyl having from 1-10 carbon atoms, alkanoyl having from 2-10 carbon atoms, or aroyl having from 7-10 carbon atoms; R.sub.2 is hydrogen or alkyl having from 1-6 carbon atoms; R.sub.3 is hydrogen, alkyl having from 2-10 carbon atoms, cycloalkyl having from 3-6 carbon atoms, aryl or arylalkyl, wherein aryl moieties have from 6-10 carbon atoms; X is NH.sub.2, OH, OCH.sub.3 or OCH.sub.2 CH.sub.3 ; and salts thereof.
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