Literature DB >> 26487916

Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.

Jing Zhang1, Qingyi Yang1, Jan Antoinette C Romero1, Jason Cross1, Bin Wang1, Katherine M Poutsiaka1, Felix Epie1, Douglas Bevan1, Yuchuan Wu1, Terence Moy1, Anu Daniel1, Brian Chamberlain1, Nicole Carter1, Joseph Shotwell1, Anu Arya1, Vipul Kumar1, Jared Silverman1, Kien Nguyen1, Chester A Metcalf1, Dominic Ryan1, Blaise Lippa1, Roland E Dolle1.   

Abstract

Antibacterials with a novel mechanism of action offer a great opportunity to combat widespread antimicrobial resistance. Bacterial DNA Gyrase is a clinically validated target. Through physiochemical property optimization of a pyrazolopyridone hit, a novel class of GyrB inhibitors were discovered. Guided by structure-based drug design, indazole derivatives with excellent enzymatic and antibacterial activity as well as great animal efficacy were discovered.

Entities:  

Keywords:  Antibacterial; GyrB; MRSA; indazole; topoisomerase

Year:  2015        PMID： 26487916      PMCID： PMC4601062          DOI： 10.1021/acsmedchemlett.5b00266

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  11 in total

Review 1.  Discovery and development of ATPase inhibitors of DNA gyrase as antibacterial agents.

Authors:  Marko Oblak; Miha Kotnik; Tom Solmajer
Journal:  Curr Med Chem       Date:  2007       Impact factor: 4.530

2.  Discovery of pyrazolthiazoles as novel and potent inhibitors of bacterial gyrase.

Authors:  Steven M Ronkin; Michael Badia; Steve Bellon; Anne-Laure Grillot; Christian H Gross; Trudy H Grossman; Nagraj Mani; Jonathan D Parsons; Dean Stamos; Martin Trudeau; Yunyi Wei; Paul S Charifson
Journal:  Bioorg Med Chem Lett       Date:  2010-03-15       Impact factor: 2.823

3.  A new DNA gyrase inhibitor subclass of the cyclothialidine family based on a bicyclic dilactam-lactone scaffold. Synthesis and antibacterial properties.

Authors:  Peter Angehrn; Erwin Goetschi; Hans Gmuender; Paul Hebeisen; Michael Hennig; Bernd Kuhn; Thomas Luebbers; Peter Reindl; Fabienne Ricklin; Anne Schmitt-Hoffmann
Journal:  J Med Chem       Date:  2011-03-09       Impact factor: 7.446

4.  Structure-activity relationship (SAR): effort towards blocking N-glucuronidation of indazoles (PF-03376056) by human UGT1A enzymes.

Authors:  Kelly Rose; Young-Sun Yang; Richard Sciotti; Hongliang Cai
Journal:  Drug Metab Lett       Date:  2009-01

5.  Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationships.

Authors:  Paul S Charifson; Anne-Laure Grillot; Trudy H Grossman; Jonathan D Parsons; Michael Badia; Steve Bellon; David D Deininger; Joseph E Drumm; Christian H Gross; Arnaud LeTiran; Yusheng Liao; Nagraj Mani; David P Nicolau; Emanuele Perola; Steven Ronkin; Dean Shannon; Lora L Swenson; Qing Tang; Pamela R Tessier; Ski-Kai Tian; Martin Trudeau; Tiansheng Wang; Yunyi Wei; Hong Zhang; Dean Stamos
Journal:  J Med Chem       Date:  2008-08-09       Impact factor: 7.446

Review 6.  Prospects for developing new antibacterials targeting bacterial type IIA topoisomerases.

Authors:  Tihomir Tomašić; Lucija Peterlin Mašič
Journal:  Curr Top Med Chem       Date:  2014       Impact factor: 3.295

7.  5-(2-Pyrimidinyl)-imidazo[1,2-a]pyridines are antibacterial agents targeting the ATPase domains of DNA gyrase and topoisomerase IV.

Authors:  Jeremy T Starr; Richard J Sciotti; Debra L Hanna; Michael D Huband; Lisa M Mullins; Hongliang Cai; Jeffrey W Gage; Mandy Lockard; Mark R Rauckhorst; Robert M Owen; Manjinder S Lall; Mark Tomilo; Huifen Chen; Sandra P McCurdy; Michael R Barbachyn
Journal:  Bioorg Med Chem Lett       Date:  2009-08-03       Impact factor: 2.823

8.  The nature of inhibition of DNA gyrase by the coumarins and the cyclothialidines revealed by X-ray crystallography.

Authors:  R J Lewis; O M Singh; C V Smith; T Skarzynski; A Maxwell; A J Wonacott; D B Wigley
Journal:  EMBO J       Date:  1996-03-15       Impact factor: 11.598

Review 9.  Exploiting bacterial DNA gyrase as a drug target: current state and perspectives.

Authors:  Frédéric Collin; Shantanu Karkare; Anthony Maxwell
Journal:  Appl Microbiol Biotechnol       Date:  2011-09-09       Impact factor: 4.813

10.  Tricyclic GyrB/ParE (TriBE) inhibitors: a new class of broad-spectrum dual-targeting antibacterial agents.

Authors:  Leslie W Tari; Xiaoming Li; Michael Trzoss; Daniel C Bensen; Zhiyong Chen; Thanh Lam; Junhu Zhang; Suk Joong Lee; Grayson Hough; Doug Phillipson; Suzanne Akers-Rodriguez; Mark L Cunningham; Bryan P Kwan; Kirk J Nelson; Amanda Castellano; Jeff B Locke; Vickie Brown-Driver; Timothy M Murphy; Voon S Ong; Chris M Pillar; Dean L Shinabarger; Jay Nix; Felice C Lightstone; Sergio E Wong; Toan B Nguyen; Karen J Shaw; John Finn
Journal:  PLoS One       Date:  2013-12-26       Impact factor: 3.240
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  5 in total

1.  cis-Tetrachlorido-bis(indazole)osmium(iv) and its osmium(iii) analogues: paving the way towards the cis-isomer of the ruthenium anticancer drugs KP1019 and/or NKP1339.

Authors:  Gabriel E Büchel; Susanne Kossatz; Ahmad Sadique; Peter Rapta; Michal Zalibera; Lukas Bucinsky; Stanislav Komorovsky; Joshua Telser; Jörg Eppinger; Thomas Reiner; Vladimir B Arion
Journal:  Dalton Trans       Date:  2017-09-12       Impact factor: 4.390

2.  Discovery of Pyrazolopyridones as a Novel Class of Gyrase B Inhibitors Using Structure Guided Design.

Authors:  Jason B Cross; Jing Zhang; Qingyi Yang; Michael F Mesleh; Jan Antoinette C Romero; Bin Wang; Doug Bevan; Katherine M Poutsiaka; Felix Epie; Terence Moy; Anu Daniel; Joseph Shotwell; Brian Chamberlain; Nicole Carter; Ole Andersen; John Barker; M Dominic Ryan; Chester A Metcalf; Jared Silverman; Kien Nguyen; Blaise Lippa; Roland E Dolle
Journal:  ACS Med Chem Lett       Date:  2016-02-16       Impact factor: 4.345

3.  Synthesis and biological evaluation against Leishmania donovani of novel hybrid molecules containing indazole-based 2-pyrone scaffolds.

Authors:  M El Ghozlani; L Bouissane; M Berkani; S Mojahidi; A Allam; C Menendez; S Cojean; P M Loiseau; M Baltas; E M Rakib
Journal:  Medchemcomm       Date:  2018-11-19       Impact factor: 3.597

Review 4.  Targeting DNA Replication and Repair for the Development of Novel Therapeutics against Tuberculosis.

Authors:  Michael A Reiche; Digby F Warner; Valerie Mizrahi
Journal:  Front Mol Biosci       Date:  2017-11-14

5.  New N-phenylpyrrolamide DNA gyrase B inhibitors: Optimization of efficacy and antibacterial activity.

Authors:  Martina Durcik; Denise Lovison; Žiga Skok; Cristina Durante Cruz; Päivi Tammela; Tihomir Tomašič; Davide Benedetto Tiz; Gábor Draskovits; Ákos Nyerges; Csaba Pál; Janez Ilaš; Lucija Peterlin Mašič; Danijel Kikelj; Nace Zidar
Journal:  Eur J Med Chem       Date:  2018-05-10       Impact factor: 6.514
  5 in total

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