Literature DB >> 14592513

Structure-activity relationship of benzo[b]thiophene-2-sulfonamide derivatives as novel human chymase inhibitors.

Hidekazu Masaki1, Yusuke Mizuno, Akira Tatui, Akira Murakami, Yuuki Koide, Shoji Satoh, Atsuo Takahashi.   

Abstract

We have identified a new class of chymase inhibitor through a substituent analysis of MWP00965, which we previously discovered by in silico screening. TY-51076 (7) showed high potency (IC(50)=56 nM) and excellent selectivity for chymase compared to chymotrypsin and cathepsin G (>400-fold). The synthesis and structure-activity relationship of this class are described.

Entities:  

Mesh:

Substances:

Year:  2003        PMID: 14592513     DOI: 10.1016/j.bmcl.2003.08.040

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


  3 in total

Review 1.  Novel Insight into the in vivo Function of Mast Cell Chymase: Lessons from Knockouts and Inhibitors.

Authors:  Gunnar Pejler
Journal:  J Innate Immun       Date:  2020-06-04       Impact factor: 7.349

2.  Expression of recombinant human mast cell chymase with Asn-linked glycans in glycoengineered Pichia pastoris.

Authors:  Eliot T Smith; Evan T Perry; Megan B Sears; David A Johnson
Journal:  Protein Expr Purif       Date:  2014-08-12       Impact factor: 1.650

3.  Molecular modeling study for inhibition mechanism of human chymase and its application in inhibitor design.

Authors:  Mahreen Arooj; Songmi Kim; Sugunadevi Sakkiah; Guang Ping Cao; Yuno Lee; Keun Woo Lee
Journal:  PLoS One       Date:  2013-04-25       Impact factor: 3.240

  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.