| 摘要 |
<p>Certain 4-substituted-3-peptidyl-azetidin-2-one compounds exhibit excellent cysteine proteinase inhibitory activity which can be used in the treatment of different diseases such as muscular dystrophy, bone resorption, myocardial infarction and cancer metastasis. These compounds are 4-substituted-3-peptidyl-azetidin-2-ones of formula (I) or pharmaceutically acceptable salts thereof, wherein R1 is hydrogen; C1-C6 alkyl which is unsubstituted or substituted; R2 is selected from the group consisting of hydrogen; C1-C6 alkyl which is unsubstituted or substituted; -XR6 wherein X is O, S, SO, or SO2; R6 is C1-C6 alkyl which is unsubstituted or substituted. Peptidyl group is a 1-2 amino acid residue wherein the free NH2 is unsubstituted or substituted with a protective group selected from the group consisting of aryloxy carbonyl, alkoxy carbonyl, substituted alkanoyl, arylalkanoyl, arylalkenoyl, heterocyclealkanoyl, heterocyclealkenoyl alkylsulphonyl, arylsulphonyl, arylalkanylsulphonyl, arylalkensulphonyl, heterocyclealkanylsulphonyl, heterocyclealkensulphonyl, and heteroarylsulphonyl.</p> |
