197965-90-5Relevant academic research and scientific papers
DITHIAZOLE COMPOUNDS, MATRIX METALLOPROTEASE INHIBITORS AND EXTERNAL PREPARATIONS FOR THE SKIN
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Page 36, (2008/06/13)
A dithiazole compound or a salt thereof expressed by formula (I): wherein R1, is hydrogen atom, alkyl, etc.; R2 is hydrogen atom, hydroxy, alkyl, aryl, arylalkoxy, arylalkyl, etc.; R3 is one group of formulae (II), (III) and (IV): This compound has an excellent inhibiting action on matrix metalloprotease (MMPs) activity, and is useful for pharmaceutical, cosmetic and skin external compositions.
Discovery of CGS 27023A, a non, peptidic, potent, and orally active stromelysin inhibitor that blocks cartilage degradation in rabbits
MacPherson, Lawrence J.,Bayburt, Erol K.,Capparelli, Michael P.,Carroll, Brian J.,Goldstein, Robert,Justice, Michael R.,Zhu, Lijuan,Hu, Shou-Ih,Melton, Richard A.,Fryer, Lynn,Goldberg, Ron L.,Doughty, John R.,Spirito, Salvatore,Blancuzzi, Vincent,Wilson, Doug,O'Byrne, Elizabeth M.,Ganu, Vishwas,Parker, David T.
, p. 2525 - 2532 (2007/10/03)
Structure-activity relationships of a lead hydroxamic acid inhibitor of recombinant human stromelysin were systematically defined by taking advantage of a concise synthesis that allowed diverse functionality to be explored at each position in a template. An ex vivo rat model and an in vivo rabbit model of stromelysin-induced cartilage degradation were used to further optimize these analogs for oral activity and duration of action. The culmination of these modifications resulted in CGS 27023A, a potent, orally active stromelysin inhibitor that blocks the erosion of cartilage matrix.
