Literature DB >> 27055939

Novel tricyclics (e.g., GSK945237) as potent inhibitors of bacterial type IIA topoisomerases.

Timothy J Miles1, Alan J Hennessy2, Ben Bax3, Gerald Brooks4, Barry S Brown5, Pamela Brown2, Nathalie Cailleau4, Dongzhao Chen5, Steven Dabbs2, David T Davies4, Joel M Esken5, Ilaria Giordano6, Jennifer L Hoover5, Graham E Jones4, Senthill K Kusalakumari Sukmar5, Roger E Markwell4, Elisabeth A Minthorn7, Steve Rittenhouse5, Michael N Gwynn5, Neil D Pearson5.   

Abstract

During the course of our research on the lead optimisation of the NBTI (Novel Bacterial Type II Topoisomerase Inhibitors) class of antibacterials, we discovered a series of tricyclic compounds that showed good Gram-positive and Gram-negative potency. Herein we will discuss the various subunits that were investigated in this series and report advanced studies on compound 1 (GSK945237) which demonstrates good PK and in vivo efficacy properties.
Copyright © 2016 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Antibacterials; Bacterial type IIA topoisomerase; GSK945237; In vivo efficacy; NBTI; Pharmacokinetic; Tricyclics

Mesh：

Substances：

Year:  2016        PMID： 27055939     DOI： 10.1016/j.bmcl.2016.03.106

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


  15 in total

1.  Bimodal Actions of a Naphthyridone/Aminopiperidine-Based Antibacterial That Targets Gyrase and Topoisomerase IV.

Authors:  Elizabeth G Gibson; Alexandria A Oviatt; Monica Cacho; Keir C Neuman; Pan F Chan; Neil Osheroff
Journal:  Biochemistry       Date:  2019-10-28       Impact factor: 3.162

2.  Rapid Evolution of Reduced Susceptibility against a Balanced Dual-Targeting Antibiotic through Stepping-Stone Mutations.

Authors:  Petra Szili; Gábor Draskovits; Tamás Révész; Ferenc Bogár; Dávid Balogh; Tamás Martinek; Lejla Daruka; Réka Spohn; Bálint Márk Vásárhelyi; Márton Czikkely; Bálint Kintses; Gábor Grézal; Györgyi Ferenc; Csaba Pál; Ákos Nyerges
Journal:  Antimicrob Agents Chemother       Date:  2019-08-23       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.  Mechanistic and Structural Basis for the Actions of the Antibacterial Gepotidacin against Staphylococcus aureus Gyrase.

Authors:  Elizabeth G Gibson; Ben Bax; Pan F Chan; Neil Osheroff
Journal:  ACS Infect Dis       Date:  2019-02-28       Impact factor: 5.084

5.  Novel Bacterial Topoisomerase Inhibitors with Potent Broad-Spectrum Activity against Drug-Resistant Bacteria.

Authors:  Cédric Charrier; Anne-Marie Salisbury; Victoria J Savage; Thomas Duffy; Emmanuel Moyo; Nathan Chaffer-Malam; Nicola Ooi; Rebecca Newman; Jonathan Cheung; Richard Metzger; David McGarry; Mark Pichowicz; Ralph Sigerson; Ian R Cooper; Gary Nelson; Hayley S Butler; Mark Craighead; Andrew J Ratcliffe; Stuart A Best; Neil R Stokes
Journal:  Antimicrob Agents Chemother       Date:  2017-04-24       Impact factor: 5.191

6.  1,3-Dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Expanding Structural Diversity and the Antibacterial Spectrum.

Authors:  Yanran Lu; Chelsea A Mann; Sheri Nolan; Jessica A Collins; Elizabeth Parker; Jonathan Papa; Sandip Vibhute; Seyedehameneh Jahanbakhsh; Mary Thwaites; David Hufnagel; Manzour H Hazbón; Jane Moreno; Timothy T Stedman; Thomas Wittum; Daniel J Wozniak; Neil Osheroff; Jack C Yalowich; Mark J Mitton-Fry
Journal:  ACS Med Chem Lett       Date:  2022-05-09       Impact factor: 4.632

Review 7.  A review on the synthesis of heteroannulated quinolones and their biological activities.

Authors:  Yaseen A M M Elshaier; Ashraf A Aly; Mohamed Abd El-Aziz; Hazem M Fathy; Alan B Brown; Mohamed Ramadan
Journal:  Mol Divers       Date:  2021-10-26       Impact factor: 3.364

8.  Thiophene antibacterials that allosterically stabilize DNA-cleavage complexes with DNA gyrase.

Authors:  Pan F Chan; Thomas Germe; Benjamin D Bax; Jianzhong Huang; Reema K Thalji; Eric Bacqué; Anna Checchia; Dongzhao Chen; Haifeng Cui; Xiao Ding; Karen Ingraham; Lynn McCloskey; Kaushik Raha; Velupillai Srikannathasan; Anthony Maxwell; Robert A Stavenger
Journal:  Proc Natl Acad Sci U S A       Date:  2017-05-15       Impact factor: 11.205

9.  Antibacterial small molecules targeting the conserved TOPRIM domain of DNA gyrase.

Authors:  Scott S Walker; Marc Labroli; Ronald E Painter; Judyann Wiltsie; Brad Sherborne; Nicholas Murgolo; Xinwei Sher; Paul Mann; Paul Zuck; Charles G Garlisi; Jing Su; Stacia Kargman; Li Xiao; Giovanna Scapin; Scott Salowe; Kristine Devito; Payal Sheth; Nichole Buist; Christopher M Tan; Todd A Black; Terry Roemer
Journal:  PLoS One       Date:  2017-07-10       Impact factor: 3.240

10.  Producing irreversible topoisomerase II-mediated DNA breaks by site-specific Pt(II)-methionine coordination chemistry.

Authors:  Ying-Ren Wang; Shin-Fu Chen; Chyuan-Chuan Wu; Yi-Wen Liao; Te-Sheng Lin; Ko-Ting Liu; Yi-Song Chen; Tsai-Kun Li; Tun-Cheng Chien; Nei-Li Chan
Journal:  Nucleic Acids Res       Date:  2017-10-13       Impact factor: 16.971
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