Literature DB >> 15911249

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

Corey R Hopkins1, Mark Czekaj, Steven S Kaye, Zhongli Gao, James Pribish, Henry Pauls, Guyan Liang, Keith Sides, Dona Cramer, Jennifer Cairns, Yongyi Luo, Heng-Keang Lim, Roy Vaz, Sam Rebello, Sebastian Maignan, Alain Dupuy, Magali Mathieu, Julian Levell.   

Abstract

A new series of novel mast cell tryptase inhibitors is reported, which features the use of an indole structure as the hydrophobic substituent on a m-benzylaminepiperidine template. The best members of this series display good in vitro activity and excellent selectivity against other serine proteases.

Entities:  

Mesh:

Substances:

Year:  2005        PMID: 15911249     DOI: 10.1016/j.bmcl.2005.04.002

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Virtual Screening and X-ray Crystallography for Human Kallikrein 6 Inhibitors with an Amidinothiophene P1 Group.

Authors:  Guyan Liang; Xin Chen; Suzanne Aldous; Su-Fen Pu; Shujaath Mehdi; Elaine Powers; Andrew Giovanni; Sathapana Kongsamut; Tianhui Xia; Ying Zhang; Rachel Wang; Zhongli Gao; Gregory Merriman; Larry R McLean; Isabelle Morize
Journal:  ACS Med Chem Lett       Date:  2012-01-11       Impact factor: 4.345

  1 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.