Literature DB >> 19683922

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

Jeremy T Starr1, 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.   

Abstract

Dual inhibitors of bacterial gyrB and parE based on a 5-(2-pyrimidinyl)-imidazo[1,2-a]pyridine template exhibited MICs (microg/mL) of 0.06-64 (Sau), 0.25-64 (MRSA), 0.06-64 (Spy), 0.06-64 (Spn), and 0.03-64 (FQR Spn). Selected examples were efficacious in mouse sepsis and lung infection models at <50mg/kg (PO dosing).

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Year:  2009        PMID: 19683922     DOI: 10.1016/j.bmcl.2009.07.141

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


  7 in total

Review 1.  Challenges of antibacterial discovery.

Authors:  Lynn L Silver
Journal:  Clin Microbiol Rev       Date:  2011-01       Impact factor: 26.132

2.  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

3.  The challenge of developing robust drugs to overcome resistance.

Authors:  Amy C Anderson; Michael P Pollastri; Celia A Schiffer; Norton P Peet
Journal:  Drug Discov Today       Date:  2011-07-19       Impact factor: 7.851

4.  Biological evaluation of benzothiazole ethyl urea inhibitors of bacterial type II topoisomerases.

Authors:  Neil R Stokes; Helena B Thomaides-Brears; Stephanie Barker; James M Bennett; Joanne Berry; Ian Collins; Lloyd G Czaplewski; Vicki Gamble; Paul Lancett; Alastair Logan; Christopher J Lunniss; Hilary Peasley; Stéphanie Pommier; Daniel Price; Carol Smee; David J Haydon
Journal:  Antimicrob Agents Chemother       Date:  2013-09-16       Impact factor: 5.191

5.  Fully automated continuous flow synthesis of highly functionalized imidazo[1,2-a] heterocycles.

Authors:  Ananda Herath; Russell Dahl; Nicholas D P Cosford
Journal:  Org Lett       Date:  2010-02-05       Impact factor: 6.005

6.  Synthesis, biological evaluation and molecular docking studies of 6-(4-nitrophenoxy)-1H-imidazo[4,5-b]pyridine derivatives as novel antitubercular agents: future DprE1 inhibitors.

Authors:  Jineetkumar Gawad; Chandrakant Bonde
Journal:  Chem Cent J       Date:  2018-12-19       Impact factor: 4.215

7.  Efficient and "Green" Synthetic Route to Imidazo[1,2-a]pyridine by Cu(II)-Ascorbate-Catalyzed A3-Coupling in Aqueous Micellar Media.

Authors:  Zigmee T Bhutia; Dharmendra Das; Amrita Chatterjee; Mainak Banerjee
Journal:  ACS Omega       Date:  2019-03-01
  7 in total

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