PMID

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Solid-phase synthesis of benzisothiazolones as serine protease inhibitors.

Bristol-Myers Squibb Pharmaceutical Research Institute

Discovery of non-competitive thrombin inhibitor derived from competitive tryptase inhibitor skeleton: Shift in molecular recognition resulted from skeletal conversion of carboxylate into phosphonate.

Tokyo University of Pharmacy and Life Sciences

Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors.

Celera Genomics

Development of activity-based probes for trypsin-family serine proteases.

Celera Genomics

Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.

University of Florida

Potent, small-molecule inhibitors of human mast cell tryptase. Antiasthmatic action of a dipeptide-based transition-state analogue containing a benzothiazole ketone.

Johnson & Johnson Pharmaceutical Research & Development

Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.

The Bristol-Myers Squibb Pharmaceutical Research Institute

Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors.

Celera Genomics

Design of novel, potent, and selective human beta-tryptase inhibitors based on alpha-keto-[1,2,4]-oxadiazoles.

Celera

Synthesis and evaluation of 4-substituted benzylamine derivatives as beta-tryptase inhibitors.

Mochida Pharmaceutical

Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase.

Aventis Pharmaceuticals

Combinatorial approaches towards the discovery of new tryptase inhibitors.

University of Barcelona

Design of bivalent ligands using hydrogen bond linkers: synthesis and evaluation of inhibitors for human beta-tryptase.

Aventis Pharmaceuticals

Novel pyrazinone inhibitors of mast cell tryptase: synthesis and SAR evaluation.

Aventis Pharmaceuticals

Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase.

The Bristol-Myers Squibb Pharmaceutical Research Institute

Synthesis of potent and selective 2-azepanone inhibitors of human tryptase.

The Bristol-Myers Squibb Pharmaceutical Research Institute

Bivalent inhibition of beta-tryptase: distance scan of neighboring subunits by dibasic inhibitors.

Institut FüR Biochemie

Monocharged inhibitors of mast cell tryptase derived from potent and selective dibasic inhibitors.

Axys Pharmaceuticals

Dibasic inhibitors of human mast cell tryptase. Part 3: identification of a series of potent and selective inhibitors containing the benzamidine functionality.

Axys Pharmaceuticals

Dibasic inhibitors of human mast cell tryptase. Part 2: structure-activity relationships and requirements for potent activity.

Axys Pharmaceuticals

Dibasic inhibitors of human mast cell tryptase. Part 1: synthesis and optimization of a novel class of inhibitors.

Axys Pharmaceuticals

Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.

Roche Pharma Research and Early Development

Syntheses and evaluation of amidinobenzofuran derivatives as tryptase inhibitors.

Yoshitomi Pharmaceutical Industries

Design, Synthesis, and Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway.

Novartis Institutes For Biomedical Research

Highly efficient and versatile synthesis of libraries of constrained beta-strand mimetics.

Molecumetics