title: 6-Acylamino-penam derivatives: synthesis and inhibition of cathepsins B, L, K, and S.
abstract: The synthesis of a new series of 6-acylamino penam derivatives and their inhibition of cysteine proteases cathepsins B, L, K, and S is described. The 6-acylamino-penam sulfone compounds showed excellent cathepsin L, K, and S inhibition activity with IC(50) values in the nanomolar and subnanomolar range.
authors.affiliation: SynPhar Laboratories, currently NAEJA Pharmaceutical Inc., Edmonton, Alberta, Canada.
authors.forename: Nian E
authors.initials: NE
authors.lastname: Zhou
authors.forename: Jadwiga
authors.initials: J
authors.lastname: Kaleta
authors.forename: Enrico
authors.initials: E
authors.lastname: Purisima
authors.forename: Robert
authors.initials: R
authors.lastname: Menard
authors.forename: Ronald G
authors.initials: RG
authors.lastname: Micetich
authors.forename: Rajeshwar
authors.initials: R
authors.lastname: Singh
mesh_terms: D000588:Amines / Q000737:chemistry*; D002403:Cathepsins / Q000037:antagonists & inhibitors*; D015853:Cysteine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D007769:Lactams / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000588:Amines; D015853:Cysteine Proteinase Inhibitors; D007769:Lactams; D013450:Sulfones; C027434:4-oxa-1-azabicyclo(3.2.0)heptan-7-one; D002403:Cathepsins