Literature DB >> 20356737

Discovery of pyrazolthiazoles as novel and potent inhibitors of bacterial gyrase.

Steven M Ronkin1, Michael Badia, Steve Bellon, Anne-Laure Grillot, Christian H Gross, Trudy H Grossman, Nagraj Mani, Jonathan D Parsons, Dean Stamos, Martin Trudeau, Yunyi Wei, Paul S Charifson.   

Abstract

Bacterial DNA gyrase is an attractive target for the investigation of new antibacterial agents. Inhibitors of the GyrB subunit, which contains the ATP-binding site, are described in this communication. Novel, substituted 5-(1H-pyrazol-3-yl)thiazole compounds were identified as inhibitors of bacterial gyrase. Structure-guided optimization led to greater enzymatic potency and moderate antibacterial potency. Data are presented for the demonstration of selective enzyme inhibition of Escherichia coli GyrB over Staphylococcus aureus GyrB. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20356737     DOI： 10.1016/j.bmcl.2010.03.052

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


  9 in total

1.  Thermodynamic computational approach to capture molecular recognition in the binding of different inhibitors to the DNA gyrase B subunit from Escherichia coli.

Authors:  Liane Saíz-Urra; Miguel Ángel Cabrera Pérez; Matheus Froeyen
Journal:  J Mol Model       Date:  2013-04-30       Impact factor: 1.810

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.  Role of unique loops in oligomerization and ATPase function of Plasmodium falciparum gyrase B.

Authors:  Monica Purushothaman; Suman Kumar Dhar; Ramanathan Natesh
Journal:  Protein Sci       Date:  2021-11-06       Impact factor: 6.725

4.  Novel Thiadiazole-Based Molecules as Promising Inhibitors of Black Fungi and Pathogenic Bacteria: In Vitro Antimicrobial Evaluation and Molecular Docking Studies.

Authors:  Huda R M Rashdan; Mohamad T Abdelrahman; Ihsan A Shehadi; Sara S El-Tanany; Bahaa A Hemdan
Journal:  Molecules       Date:  2022-06-04       Impact factor: 4.927

5.  Molecular docking and inhibition studies on the interactions of Bacopa monnieri's potent phytochemicals against pathogenic Staphylococcus aureus.

Authors:  Talha Bin Emran; Md Atiar Rahman; Mir Muhammad Nasir Uddin; Raju Dash; Md Firoz Hossen; Mohammad Mohiuddin; Md Rashadul Alam
Journal:  Daru       Date:  2015-04-17       Impact factor: 3.117

6.  Induction of Antibacterial Metabolites by Co-Cultivation of Two Red-Sea-Sponge-Associated Actinomycetes Micromonospora sp. UR56 and Actinokinespora sp. EG49.

Authors:  Mohamed S Hifnawy; Hossam M Hassan; Rabab Mohammed; Mohamed M Fouda; Ahmed M Sayed; Ahmed A Hamed; Sameh F AbouZid; Mostafa E Rateb; Hani A Alhadrami; Usama Ramadan Abdelmohsen
Journal:  Mar Drugs       Date:  2020-05-05       Impact factor: 5.118

7.  Targeted Isolation of Antibiotic Brominated Alkaloids from the Marine Sponge Pseudoceratina durissima Using Virtual Screening and Molecular Networking.

Authors:  James Lever; Florian Kreuder; Jason Henry; Andrew Hung; Pierre-Marie Allard; Robert Brkljača; Colin Rix; Aya C Taki; Robin B Gasser; Jan Kaslin; Donald Wlodkowic; Jean-Luc Wolfender; Sylvia Urban
Journal:  Mar Drugs       Date:  2022-08-29       Impact factor: 6.085

8.  Discovery of Two Brominated Oxindole Alkaloids as Staphylococcal DNA Gyrase and Pyruvate Kinase Inhibitors via Inverse Virtual Screening.

Authors:  Ahmed M Sayed; Hani A Alhadrami; Seham S El-Hawary; Rabab Mohammed; Hossam M Hassan; Mostafa E Rateb; Usama Ramadan Abdelmohsen; Walid Bakeer
Journal:  Microorganisms       Date:  2020-02-20

9.  Antibacterial, Antifungal, and Antioxidant Activities of Silver Nanoparticles Biosynthesized from Bauhinia tomentosa Linn.

Authors:  Senthil Renganathan; Sugunakala Subramaniyan; Nivetha Karunanithi; Preethi Vasanthakumar; Arne Kutzner; Pok-Son Kim; Klaus Heese
Journal:  Antioxidants (Basel)       Date:  2021-12-07
  9 in total

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