Literature DB >> 27096044

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

Jason B Cross1, Jing Zhang1, Qingyi Yang1, Michael F Mesleh1, Jan Antoinette C Romero1, Bin Wang1, Doug Bevan1, Katherine M Poutsiaka1, Felix Epie1, Terence Moy1, Anu Daniel1, Joseph Shotwell1, Brian Chamberlain1, Nicole Carter1, Ole Andersen2, John Barker2, M Dominic Ryan1, Chester A Metcalf1, Jared Silverman1, Kien Nguyen1, Blaise Lippa1, Roland E Dolle1.   

Abstract

The ATPase subunit of DNA gyrase B is an attractive antibacterial target due to high conservation across bacteria and the essential role it plays in DNA replication. A novel class of pyrazolopyridone inhibitors was discovered by optimizing a fragment screening hit scaffold using structure guided design. These inhibitors show potent Gram-positive antibacterial activity and low resistance incidence against clinically important pathogens.

Entities:  

Keywords:  Antibacterials; DNA gyrase B; fragment-based drug design; structure-based drug design

Year:  2016        PMID： 27096044      PMCID： PMC4834655          DOI： 10.1021/acsmedchemlett.5b00368

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


  14 in total

Review 1.  DNA topoisomerases: structure, function, and mechanism.

Authors:  J J Champoux
Journal:  Annu Rev Biochem       Date:  2001       Impact factor: 23.643

2.  Pyrrolamide DNA gyrase inhibitors: optimization of antibacterial activity and efficacy.

Authors:  Brian A Sherer; Kenneth Hull; Oluyinka Green; Gregory Basarab; Sheila Hauck; Pamela Hill; James T Loch; George Mullen; Shanta Bist; Joanna Bryant; Ann Boriack-Sjodin; Jon Read; Nancy DeGrace; Maria Uria-Nickelsen; Ruth N Illingworth; Ann E Eakin
Journal:  Bioorg Med Chem Lett       Date:  2011-10-12       Impact factor: 2.823

3.  Dual targeting of GyrB and ParE by a novel aminobenzimidazole class of antibacterial compounds.

Authors:  Trudy H Grossman; Douglas J Bartels; Steve Mullin; Christian H Gross; Jonathan D Parsons; Yusheng Liao; Anne-Laure Grillot; Dean Stamos; Eric R Olson; Paul S Charifson; Nagraj Mani
Journal:  Antimicrob Agents Chemother       Date:  2006-11-20       Impact factor: 5.191

Review 4.  Drugs for bad bugs: confronting the challenges of antibacterial discovery.

Authors:  David J Payne; Michael N Gwynn; David J Holmes; David L Pompliano
Journal:  Nat Rev Drug Discov       Date:  2006-12-08       Impact factor: 84.694

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

Authors:  Jing Zhang; Qingyi Yang; Jan Antoinette C Romero; Jason Cross; Bin Wang; Katherine M Poutsiaka; Felix Epie; Douglas Bevan; Yuchuan Wu; Terence Moy; Anu Daniel; Brian Chamberlain; Nicole Carter; Joseph Shotwell; Anu Arya; Vipul Kumar; Jared Silverman; Kien Nguyen; Chester A Metcalf; Dominic Ryan; Blaise Lippa; Roland E Dolle
Journal:  ACS Med Chem Lett       Date:  2015-09-08       Impact factor: 4.345

6.  Structure and mechanism of DNA topoisomerase II.

Authors:  J M Berger; S J Gamblin; S C Harrison; J C Wang
Journal:  Nature       Date:  1996-01-18       Impact factor: 49.962

7.  Fragment-to-hit-to-lead discovery of a novel pyridylurea scaffold of ATP competitive dual targeting type II topoisomerase inhibiting antibacterial agents.

Authors:  Gregory S Basarab; John I Manchester; Shanta Bist; P Ann Boriack-Sjodin; Brian Dangel; Ruth Illingworth; Brian A Sherer; Shubha Sriram; Maria Uria-Nickelsen; Ann E Eakin
Journal:  J Med Chem       Date:  2013-10-29       Impact factor: 7.446

8.  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

9.  Pyrrolopyrimidine inhibitors of DNA gyrase B (GyrB) and topoisomerase IV (ParE). Part I: Structure guided discovery and optimization of dual targeting agents with potent, broad-spectrum enzymatic activity.

Authors:  Leslie W Tari; Michael Trzoss; Daniel C Bensen; Xiaoming Li; Zhiyong Chen; Thanh Lam; Junhu Zhang; Christopher J Creighton; Mark L Cunningham; Bryan Kwan; Mark Stidham; Karen J Shaw; Felice C Lightstone; Sergio E Wong; Toan B Nguyen; Jay Nix; John Finn
Journal:  Bioorg Med Chem Lett       Date:  2012-12-05       Impact factor: 2.823

10.  New antibacterial agents derived from the DNA gyrase inhibitor cyclothialidine.

Authors:  Peter Angehrn; Stefan Buchmann; Christoph Funk; Erwin Goetschi; Hans Gmuender; Paul Hebeisen; Dirk Kostrewa; Helmut Link; Thomas Luebbers; Raffaello Masciadri; Joergen Nielsen; Peter Reindl; Fabienne Ricklin; Anne Schmitt-Hoffmann; Frank-Peter Theil
Journal:  J Med Chem       Date:  2004-03-11       Impact factor: 7.446
View more
  3 in total

1.  Identification of an auxiliary druggable pocket in the DNA gyrase ATPase domain using fragment probes.

Authors:  Xiaojie Huang; Junsong Guo; Qi Liu; Qiong Gu; Jun Xu; Huihao Zhou
Journal:  Medchemcomm       Date:  2018-07-04       Impact factor: 3.597

2.  New N-phenyl-4,5-dibromopyrrolamides as DNA gyrase B inhibitors.

Authors:  Nace Zidar; Helena Macut; Tihomir Tomašič; Lucija Peterlin Mašič; Janez Ilaš; Anamarija Zega; Päivi Tammela; Danijel Kikelj
Journal:  Medchemcomm       Date:  2019-05-20       Impact factor: 3.597

3.  A regioselective C7 bromination and C7 palladium-catalyzed Suzuki-Miyaura cross-coupling arylation of 4-substituted NH-free indazoles.

Authors:  Khalid Boujdi; Nabil El Brahmi; Jérôme Graton; Didier Dubreuil; Sylvain Collet; Monique Mathé-Allainmat; Mohamed Akssira; Jacques Lebreton; Saïd El Kazzouli
Journal:  RSC Adv       Date:  2021-02-10       Impact factor: 3.361
  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.