Bioorganic & Medicinal Chemistry Letters 2000-10-16

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

K D Rice, A R Gangloff, E Y Kuo, J M Dener, V R Wang, R Lum, W S Newcomb, C Havel, D Putnam, L Cregar, M Wong, R L Warne

Index: Bioorg. Med. Chem. Lett. 10(20) , 2357-60, (2000)

Full Text: HTML

Abstract

The synthesis and optimization of a novel class of reversible and active-site directed dibasic inhibitors of human mast cell tryptase are described. The compounds were shown to be both remarkably potent and selective for tryptase with Ki values for optimized inhibitors in the picomolar range.

Related Compounds

  • m-Xylylenediamine

Related Articles:

Prick testing with chemicals in the diagnosis of occupational contact urticaria and respiratory diseases.

2015-01-01

[Contact Dermatitis 72(1) , 20-32, (2014)]

New efficient substrates for semicarbazide-sensitive amine oxidase/VAP-1 enzyme: analysis by SARs and computational docking.

2006-10-19

[J. Med. Chem. 49 , 6197-208, (2006)]

Oxidative DNA cleavage promoted by multinuclear copper complexes: activity dependence on the complex structure.

2006-08-25

[Chemistry 12(25) , 6621-9, (2006)]

An attempt to improve diagnostics of contact allergy due to epoxy resin systems. First results of the multicentre study EPOX 2002.

2004-01-01

[Contact Dermatitis 51(5-6) , 263-72, (2004)]

Overall migration and specific migration of bisphenol A diglycidyl ether monomer and m-xylylenediamine hardener from an optimized epoxy-amine formulation into water-based food simulants.

1993-01-01

[Food Addit. Contam. 10(5) , 555-65, (1993)]

More Articles...