Literature DB >> 22030032

Novel cyclohexyl-amides as potent antibacterials targeting bacterial type IIA topoisomerases.

Timothy J Miles1, Christopher Barfoot, Gerald Brooks, Pamela Brown, Dongzhao Chen, Steven Dabbs, David T Davies, David L Downie, Susanne Eyrisch, Ilaria Giordano, Michael N Gwynn, Alan Hennessy, Jennifer Hoover, Jianzhong Huang, Graham Jones, Roger Markwell, Stephen Rittenhouse, Hong Xiang, Neil Pearson.   

Abstract

As part of our wider efforts to exploit novel mode of action antibacterials, we have discovered a series of cyclohexyl-amide compounds that has good Gram positive and Gram negative potency. The mechanism of action is via inhibition of bacterial topoisomerases II and IV. We have investigated various subunits in this series and report advanced studies on compound 7 which demonstrates good PK and in vivo efficacy properties.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 22030032     DOI: 10.1016/j.bmcl.2011.09.114

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


  8 in total

1.  In Vitro and In Vivo Characterization of the Novel Oxabicyclooctane-Linked Bacterial Topoisomerase Inhibitor AM-8722, a Selective, Potent Inhibitor of Bacterial DNA Gyrase.

Authors:  Christopher M Tan; Charles J Gill; Jin Wu; Nathalie Toussaint; Jingjun Yin; Takayuki Tsuchiya; Charles G Garlisi; David Kaelin; Peter T Meinke; Lynn Miesel; David B Olsen; Armando Lagrutta; Hideyuki Fukuda; Ryuta Kishii; Masaya Takei; Kouhei Oohata; Tomoko Takeuchi; Taku Shibue; Hisashi Takano; Akinori Nishimura; Yasumichi Fukuda; Sheo B Singh
Journal:  Antimicrob Agents Chemother       Date:  2016-07-22       Impact factor: 5.191

2.  Mycobacterium tuberculosis gyrase inhibitors as a new class of antitubercular drugs.

Authors:  Delia Blanco; Esther Perez-Herran; Mónica Cacho; Lluís Ballell; Julia Castro; Rubén González Del Río; José Luis Lavandera; Modesto J Remuiñán; Cindy Richards; Joaquin Rullas; María Jesús Vázquez-Muñiz; Ermias Woldu; María Cleofé Zapatero-González; Iñigo Angulo-Barturen; Alfonso Mendoza; David Barros
Journal:  Antimicrob Agents Chemother       Date:  2015-01-12       Impact factor: 5.191

Review 3.  Topoisomerases as anticancer targets.

Authors:  Justine L Delgado; Chao-Ming Hsieh; Nei-Li Chan; Hiroshi Hiasa
Journal:  Biochem J       Date:  2018-01-23       Impact factor: 3.857

4.  Oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad spectrum antibacterial agents.

Authors:  Sheo B Singh; David E Kaelin; Jin Wu; Lynn Miesel; Christopher M Tan; Peter T Meinke; David Olsen; Armando Lagrutta; Prudence Bradley; Jun Lu; Sangita Patel; Keith W Rickert; Robert F Smith; Stephen Soisson; Changqing Wei; Hideyuki Fukuda; Ryuta Kishii; Masaya Takei; Yasumichi Fukuda
Journal:  ACS Med Chem Lett       Date:  2014-03-12       Impact factor: 4.345

5.  Structure-Activity Relationship of Anti-Mycobacterium abscessus Piperidine-4-carboxamides, a New Class of NBTI DNA Gyrase Inhibitors.

Authors:  Andreas Beuchel; Dina Robaa; Dereje A Negatu; Abdeldjalil Madani; Nadine Alvarez; Matthew D Zimmerman; Adrian Richter; Lea Mann; Sophie Hoenke; René Csuk; Thomas Dick; Peter Imming
Journal:  ACS Med Chem Lett       Date:  2022-02-28       Impact factor: 4.345

6.  A Robust Pneumonia Model in Immunocompetent Rodents to Evaluate Antibacterial Efficacy against S. pneumoniae, H. influenzae, K. pneumoniae, P. aeruginosa or A. baumannii.

Authors:  Jennifer L Hoover; Thomas F Lewandowski; Cindy L Mininger; Christine M Singley; Scott Sucoloski; Stephen Rittenhouse
Journal:  J Vis Exp       Date:  2017-01-02       Impact factor: 1.355

Review 7.  Two Decades of Successful SAR-Grounded Stories of the Novel Bacterial Topoisomerase Inhibitors (NBTIs).

Authors:  Anja Kolarič; Marko Anderluh; Nikola Minovski
Journal:  J Med Chem       Date:  2020-02-17       Impact factor: 7.446

8.  A Mycobacterium tuberculosis NBTI DNA Gyrase Inhibitor Is Active against Mycobacterium abscessus.

Authors:  Uday S Ganapathy; Rubén González Del Río; Mónica Cacho-Izquierdo; Fátima Ortega; Joël Lelièvre; David Barros-Aguirre; Wassihun Wedajo Aragaw; Matthew D Zimmerman; Marissa Lindman; Véronique Dartois; Martin Gengenbacher; Thomas Dick
Journal:  Antimicrob Agents Chemother       Date:  2021-10-04       Impact factor: 5.191

  8 in total

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