Literature DB >> 9022976

Non-peptidic inhibitors of human neutrophil elastase: the design and synthesis of sulfonanilide-containing inhibitors.

K Imaki1, T Okada, Y Nakayama, Y Nagao, K Kobayashi, Y Sakai, T Mohri, T Amino, H Nakai, M Kawamura.   

Abstract

A novel series of pivaloyloxy benzene derivatives has been identified as potent and selective human neutrophil elastase (HNE) inhibitors. Convergent syntheses were developed in order to identify the inhibitors which are intravenously effective in an animal model. A compound of particular interest is the sulfonanilide-containing analogues. Structure-activity relationships are discussed. Structural requirements for metabolic stabilization are also discussed.

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Year:  1996        PMID: 9022976     DOI: 10.1016/s0968-0896(96)00216-7

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  5 in total

1.  Structural Diversity and Anticancer Activity of Marine-Derived Elastase Inhibitors: Key Features and Mechanisms Mediating the Antimetastatic Effects in Invasive Breast Cancer.

Authors:  Fatma H Al-Awadhi; Valerie J Paul; Hendrik Luesch
Journal:  Chembiochem       Date:  2018-03-23       Impact factor: 3.164

2.  Inhibition of serine proteases by a new class of cyclosulfamide-based carbamylating agents.

Authors:  Qingliang Yang; Yi Li; Dengfeng Dou; Xiangdong Gan; Swathi Mohan; Christopher S Groutas; Laura E Stevenson; Zhong Lai; Kevin R Alliston; Jiaying Zhong; Todd D Williams; William C Groutas
Journal:  Arch Biochem Biophys       Date:  2008-04-22       Impact factor: 4.013

3.  Potent elastase inhibitors from cyanobacteria: structural basis and mechanisms mediating cytoprotective and anti-inflammatory effects in bronchial epithelial cells.

Authors:  Lilibeth A Salvador; Kanchan Taori; Jason S Biggs; Jean Jakoncic; David A Ostrov; Valerie J Paul; Hendrik Luesch
Journal:  J Med Chem       Date:  2013-01-28       Impact factor: 7.446

4.  Neutrophil Elastase Inhibition Ameliorates Endotoxin-induced Myocardial Injury Accompanying Degradation of Cardiac Capillary Glycocalyx.

Authors:  Tetsuya Fukuta; Hideshi Okada; Genzou Takemura; Kodai Suzuki; Chihiro Takada; Hiroyuki Tomita; Akio Suzuki; Kazumasa Oda; Akihiro Uchida; Saori Matsuo; Hirotsugu Fukuda; Hirohisa Yano; Isamu Muraki; Ryogen Zaikokuji; Ayumi Kuroda; Ayane Nishio; So Sampei; Nagisa Miyazaki; Yasuaki Hotta; Noriaki Yamada; Takatomo Watanabe; Kentaro Morishita; Tomoaki Doi; Takahiro Yoshida; Hiroaki Ushikoshi; Shozo Yoshida; Yoichi Maekawa; Shinji Ogura
Journal:  Shock       Date:  2020-09       Impact factor: 3.533

5.  Neutrophil Elastase Deficiency Ameliorates Myocardial Injury Post Myocardial Infarction in Mice.

Authors:  Yukino Ogura; Kazuko Tajiri; Nobuyuki Murakoshi; DongZhu Xu; Saori Yonebayashi; Siqi Li; Yuta Okabe; Duo Feng; Yuzuno Shimoda; Zoughu Song; Haruka Mori; Zixun Yuan; Kazutaka Aonuma; Masaki Ieda
Journal:  Int J Mol Sci       Date:  2021-01-13       Impact factor: 5.923

  5 in total

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