Literature DB >> 22047689

Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases.

Timothy J Miles1, Jeffrey M Axten, Christopher Barfoot, Gerald Brooks, Pamela Brown, Dongzhao Chen, Steven Dabbs, David T Davies, David L Downie, Susanne Eyrisch, Timothy Gallagher, Ilaria Giordano, Michael N Gwynn, Alan Hennessy, Jennifer Hoover, Jianzhong Huang, Graham Jones, Roger Markwell, William H Miller, Elizabeth A Minthorn, Stephen Rittenhouse, Mark Seefeld, Neil Pearson.   

Abstract

We have identified a series of amino-piperidine antibacterials with a good broad spectrum potency. We report the investigation of various subunits in this series and advanced studies on compound 8. Compound 8 possesses good pharmacokinetics, broad spectrum antibacterial activity and demonstrates oral efficacy in a rat lung infection model.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 22047689     DOI： 10.1016/j.bmcl.2011.09.117

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


  9 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.  Target-based resistance in Pseudomonas aeruginosa and Escherichia coli to NBTI 5463, a novel bacterial type II topoisomerase inhibitor.

Authors:  Asha S Nayar; Thomas J Dougherty; Folkert Reck; Jason Thresher; Ning Gao; Adam B Shapiro; David E Ehmann
Journal:  Antimicrob Agents Chemother       Date:  2014-10-27       Impact factor: 5.191

5.  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

6.  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

7.  Piperidinyl Ureas Chemically Control Defective in Cullin Neddylation 1 (DCN1)-Mediated Cullin Neddylation.

Authors:  Jared T Hammill; Daniel C Scott; Jaeki Min; Michele C Connelly; Gloria Holbrook; Fangyi Zhu; Amy Matheny; Lei Yang; Bhuvanesh Singh; Brenda A Schulman; R Kiplin Guy
Journal:  J Med Chem       Date:  2018-03-26       Impact factor: 7.446

Review 8.  The Structural Features of Novel Bacterial Topoisomerase Inhibitors That Define Their Activity on Topoisomerase IV.

Authors:  Maja Kokot; Marko Anderluh; Martina Hrast; Nikola Minovski
Journal:  J Med Chem       Date:  2022-05-03       Impact factor: 8.039

9.  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
  9 in total

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