Search

Your search keyword '"Douglas Guy"' showing total 3 results
Start Over Author "Douglas Guy" Publisher elsevier bv
3 results on '"Douglas Guy"'

1. Rapid synthesis of RGD mimetics with isoxazoline scaffolds on solid phase: Identification of αvβ3 antagonists lead compounds

Author

Douglas Guy Batt, William F. DeGrado, Arlene Rockwell, Prabhakar K. Jadhav, Joseph J. Petraitis, Shaker A. Mousa, Maria Rafalski, and William J. Pitts

Subjects
chemistry.chemical_classification, Stereochemistry, medicine.drug_class, Carboxylic acid, Molecular Mimicry, Organic Chemistry, Clinical Biochemistry, Pharmaceutical Science, Carboxamide, Isoxazoles, Biochemistry, Chemical synthesis, Sulfonamide, Chain length, chemistry, Phase (matter), Drug Discovery, Structural isomer, medicine, Molecular Medicine, Receptors, Vitronectin, Oligopeptides, Molecular Biology
Abstract

Isoxazoline containing RGD mimetics were rapidly synthesized on a solid phase to optimize linkers, regioisomers of isoxazoline scaffolds, and exosite binding groups to yield lead alphavbeta3 antagonists.

Published
1999

2. Metabolism resistant isothiazolone inhibitors of cartilage breakdown

Author

Stephen W. Wright, Douglas Guy Batt, M. A. Pratta, Joseph J. Petraitis, Ronald L. Magolda, E. C. Arner, Susan R. Sherk, John V. Giannaras, Donald Joseph-Phillip Pinto, Orwat Michael James, Ronald L. Corbett, Bruce Freimark, Jean M. Williams, Susan V. Di Meo, and Herman F. Stampfli

Subjects
Pyridines, Indomethacin, Clinical Biochemistry, Pharmaceutical Science, Matrix metalloproteinase, Organ culture, Biochemistry, Structure-Activity Relationship, Naproxen, Organ Culture Techniques, Reductive metabolism, Microsomes, Drug Discovery, Nasal septum, medicine, Animals, Molecular Biology, Nasal Septum, Chemistry, Cartilage, Organic Chemistry, Metalloendopeptidases, Metabolism, Thiazoles, medicine.anatomical_structure, Microsome, Pyrazoles, Molecular Medicine, Cattle, Matrix Metalloproteinase 3, Proteoglycans, Oxidation-Reduction, Interleukin-1
Abstract

A series of 2-(arylmethyl)pyridoisothiazolones is reported that inhibit the IL-1 β induced breakdown of bovine nasal septum cartilage in an organ culture assay. The synthesis and preliminary SAR of these compounds are described. These compounds represent a novel, non-peptide lead series approach to the mediation of the chronic cartilage breakdown associated with arthritic disease. These compounds are relatively resistant to reductive metabolism by liver microsomal preparations and appear to inhibit cartilage breakdown by interfering with the proteolytic activation of matrix metalloproteinases.

Published
1995

Catalog

Books, media, physical & digital resources
See catalog results