Literature DB >> 11425539

Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.

Y Aoyama1, M Uenaka, T Konoike, Y Hayasaki-Kajiwara, N Naya, M Nakajima.   

Abstract

The present work demonstrates that the 1,3-diazetidine-2,4-dione nucleus is effective as a scaffold of serine protease inhibitors. Compound 1 displayed high activity against human cathepsin G and alpha-chymotrypsin (0.39, 0.69 nM). Compound 6 exhibited 0.85 nM inhibition of human chymase. Compound 10 was a selective inhibitor against human neutrophil elastase.

Entities:  

Mesh：

Substances：

Year:  2001        PMID： 11425539     DOI： 10.1016/s0960-894x(01)00264-5

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


  5 in total

1.  Design, synthesis and evaluation of N-benzoylindazole derivatives and analogues as inhibitors of human neutrophil elastase.

Authors:  Letizia Crocetti; Maria Paola Giovannoni; Igor A Schepetkin; Mark T Quinn; Andrei I Khlebnikov; Agostino Cilibrizzi; Vittorio Dal Piaz; Alessia Graziano; Claudia Vergelli
Journal:  Bioorg Med Chem       Date:  2011-07-07       Impact factor: 3.641

2.  Optimization of a β-Lactam Scaffold for Antibacterial Activity via the Inhibition of Bacterial Type I Signal Peptidase.

Authors:  Chien-Hung Yeh; Shawn I Walsh; Arryn Craney; M Greg Tabor; Ana-Florina Voica; Ramkrishna Adhikary; Sydney E Morris; Floyd E Romesberg
Journal:  ACS Med Chem Lett       Date:  2018-03-15       Impact factor: 4.345

3.  A Practical Synthesis of Isocyanates from Isonitriles: Ethyl 2-Isocyanatoacetate.

Authors:  Hoang V Le; Bruce Ganem
Journal:  Organic Synth       Date:  2012-04-05

4.  A combination of receptor-based pharmacophore modeling & QM techniques for identification of human chymase inhibitors.

Authors:  Mahreen Arooj; Sugunadevi Sakkiah; Songmi Kim; Venkatesh Arulalapperumal; Keun Woo Lee
Journal:  PLoS One       Date:  2013-04-26       Impact factor: 3.240

5.  3D QSAR pharmacophore modeling, in silico screening, and density functional theory (DFT) approaches for identification of human chymase inhibitors.

Authors:  Mahreen Arooj; Sundarapandian Thangapandian; Shalini John; Swan Hwang; Jong Keun Park; Keun Woo Lee
Journal:  Int J Mol Sci       Date:  2011-12-12       Impact factor: 5.923
  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.