Literature DB >> 34095845

Rational design, synthesis and testing of novel tricyclic topoisomerase inhibitors for the treatment of bacterial infections part 2.

R Kirk1, A Ratcliffe1, G Noonan1, M Uosis-Martin1, D Lyth1, O Bardell-Cox1, J Massam1, P Schofield1, A Lyons1, D Clare1, J Maclean1, A Smith1, V Savage1, S Mohmed1, C Charrier1, A-M Salisbury1, E Moyo1, N Ooi1, N Chalam-Judge1, J Cheung1, N R Stokes1, S Best1, M Craighead1, R Armer1, A Huxley1.   

Abstract

Building on our previously-reported novel tricyclic topoisomerase inhibitors (NTTIs), we disclose the discovery of REDX07965, which has an MIC90 of 0.5 μg mL-1 against Staphylococcus aureus, favourable in vitro pharmacokinetic properties, selectivity versus human topoisomerase II and an acceptable toxicity profile. The results herein validate a rational design approach to address the urgent unmet medical need for novel antibiotics. This journal is © The Royal Society of Chemistry.

Entities:  

Year:  2020        PMID： 34095845      PMCID： PMC8126889          DOI： 10.1039/d0md00175a

Source DB:  PubMed          Journal:  RSC Med Chem        ISSN： 2632-8682


  8 in total

1.  Structure-activity relationships of 3-aminoquinazolinediones, a new class of bacterial type-2 topoisomerase (DNA gyrase and topo IV) inhibitors.

Authors:  Tuan P Tran; Edmund L Ellsworth; Joseph P Sanchez; Brian M Watson; Michael A Stier; H D Hollis Showalter; John M Domagala; Martin A Shapiro; E Themis Joannides; Stephen J Gracheck; Dai Q Nguyen; Paul Bird; Judy Yip; Anurag Sharadendu; Chan Ha; Saeed Ramezani; Xiujuan Wu; Rajeshwar Singh
Journal:  Bioorg Med Chem Lett       Date:  2006-12-15       Impact factor: 2.823

2.  Fully automated continuous flow synthesis of 4,5-disubstituted oxazoles.

Authors:  Marcus Baumann; Ian R Baxendale; Steven V Ley; Christoper D Smith; Geoffrey K Tranmer
Journal:  Org Lett       Date:  2006-11-09       Impact factor: 6.005

3.  Synthesis and antibacterial activity of the C-7 side chain of 3-aminoquinazolinediones.

Authors:  Kim M Hutchings; Tuan P Tran; Edmund L Ellsworth; Brian M Watson; Joseph P Sanchez; H D Showalter; Michael A Stier; Martin Shapiro; E Themis Joannides; Michael Huband; Dai Q Nguyen; Samarendra Maiti; Tingsheng Li; Jyoti Tailor; George Thomas; Chan Ha; Rajeshwar Singh
Journal:  Bioorg Med Chem Lett       Date:  2008-08-03       Impact factor: 2.823

4.  The BlueScreen-384 assay as an indicator of genotoxic hazard potential in early-stage drug discovery.

Authors:  Kate Simpson; Nicola Bevan; Paul Hastwell; Patrick Eidam; Poonam Shah; Elke Gogo; Steve Rees; Andrew Brown
Journal:  J Biomol Screen       Date:  2012-12-20

5.  3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.

Authors:  Edmund L Ellsworth; Tuan P Tran; H D Hollis Showalter; Joseph P Sanchez; Brian M Watson; Michael A Stier; John M Domagala; Stephen J Gracheck; E Themis Joannides; Martin A Shapiro; Steve A Dunham; Debra L Hanna; Michael D Huband; Jeffrey W Gage; Joel C Bronstein; Jia Yeu Liu; Dai Q Nguyen; Rajeshwar Singh
Journal:  J Med Chem       Date:  2006-11-02       Impact factor: 7.446

6.  In-vitro susceptibility of Streptococcus pneumoniae to the d- and l-isomers of ofloxacin: interpretive criteria and quality control limits.

Authors:  A L Barry; P C Fuchs; S D Allen; S D Brown; J H Jorgensen; F C Tenover
Journal:  J Antimicrob Chemother       Date:  1996-02       Impact factor: 5.790

7.  Biological profiling of novel tricyclic inhibitors of bacterial DNA gyrase and topoisomerase IV.

Authors:  Victoria J Savage; Cédric Charrier; Anne-Marie Salisbury; Emmanuel Moyo; Henry Forward; Nathan Chaffer-Malam; Richard Metzger; Anthony Huxley; Ralph Kirk; Mario Uosis-Martin; Gary Noonan; Sarfraz Mohmed; Stuart A Best; Andrew J Ratcliffe; Neil R Stokes
Journal:  J Antimicrob Chemother       Date:  2016-03-30       Impact factor: 5.790

8.  Bypassing fluoroquinolone resistance with quinazolinediones: studies of drug-gyrase-DNA complexes having implications for drug design.

Authors:  Karl Drlica; Arkady Mustaev; Tyrell R Towle; Gan Luan; Robert J Kerns; James M Berger
Journal:  ACS Chem Biol       Date:  2014-11-04       Impact factor: 5.100
  8 in total
  1 in total

1.  On drug discovery against infectious diseases and academic medicinal chemistry contributions.

Authors:  Yves L Janin
Journal:  Beilstein J Org Chem       Date:  2022-09-29       Impact factor: 2.544
  1 in total

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