Literature DB >> 11078187

Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors.

Y Aoyama1, M Uenaka, T Konoike, Y Iso, Y Nishitani, A Kanda, N Naya, M Nakajima.   

Abstract

1-Oxacephem derivatives were synthesized and evaluated as a novel series of chymase inhibitors. Structure-activity relationship studies of 1-oxacephems led to compound 34, which exhibited 6 nM inhibition of human chymase and high selectivity for human chymase compared to other serine enzymes.

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Year:  2000        PMID： 11078187     DOI： 10.1016/s0960-894x(00)00488-1

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


  5 in total

1.  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

2.  Penicillin Derivatives Inhibit the SARS-CoV-2 Main Protease by Reaction with Its Nucleophilic Cysteine.

Authors:  Tika R Malla; Lennart Brewitz; Dorian-Gabriel Muntean; Hiba Aslam; C David Owen; Eidarus Salah; Anthony Tumber; Petra Lukacik; Claire Strain-Damerell; Halina Mikolajek; Martin A Walsh; Christopher J Schofield
Journal:  J Med Chem       Date:  2022-05-12       Impact factor: 8.039

3.  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

4.  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.  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
  5 in total

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