2. Academic Validation
  3. Discovery of CGS 27023A, a non-peptidic, potent, and orally active stromelysin inhibitor that blocks cartilage degradation in rabbits

Discovery of CGS 27023A, a non-peptidic, potent, and orally active stromelysin inhibitor that blocks cartilage degradation in rabbits

  • J Med Chem. 1997 Aug 1;40(16):2525-32. doi: 10.1021/jm960871c.
L J MacPherson 1,  E K Bayburt,  M P Capparelli,  B J Carroll,  R Goldstein,  M R Justice,  L Zhu,  S Hu,  R A Melton,  L Fryer,  R L Goldberg,  J R Doughty,  S Spirito,  V Blancuzzi,  D Wilson,  E M O'Byrne,  V Ganu,  D T Parker
Affiliations

Affiliation

  • 1 Research Department, Novartis Pharmaceuticals, Summit, New Jersey 07901, USA.
PMID: 9258358 DOI: 10.1021/jm960871c
Abstract

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.

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