Literature DB >> 23623254

Benzimidazole-based antibacterial agents against Francisella tularensis.

Kunal Kumar1, Divya Awasthi, Seung-Yub Lee, Jason E Cummings, Susan E Knudson, Richard A Slayden, Iwao Ojima.   

Abstract

Francisella tularensis is a highly virulent pathogenic bacterium. In order to identify novel potential antibacterial agents against F. tularensis, libraries of trisubstituted benzimidazoles were screened against F. tularensis LVS strain. In a preliminary screening assay, remarkably, 23 of 2,5,6- and 2,5,7-trisubstituted benzimidazoles showed excellent activity exhibiting greater than 90% growth inhibition at 1 μg/mL. Among those hits, 21 compounds showed MIC90 values in the range of 0.35-48.6 μg/mL after accurate MIC determination. In ex vivo efficacy assays, four of these compounds exhibited 2-3log reduction in colony forming units (CFU) per mL at concentrations of 10 and 50 μg/mL.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Mesh：

Substances：

Year:  2013        PMID： 23623254      PMCID： PMC3681959          DOI： 10.1016/j.bmc.2013.02.059

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  33 in total

Review 1.  Themes and variations in prokaryotic cell division.

Authors:  W Margolin
Journal:  FEMS Microbiol Rev       Date:  2000-10       Impact factor: 16.408

2.  Tularemia: a perusal of three hundred thirty-nine cases.

Authors:  F T DIENST
Journal:  J La State Med Soc       Date:  1963-04

Review 3.  Cell-division inhibitors: new insights for future antibiotics.

Authors:  Rowena L Lock; Elizabeth J Harry
Journal:  Nat Rev Drug Discov       Date:  2008-04       Impact factor: 84.694

Review 4.  Therapeutic potential of FtsZ inhibition: a patent perspective.

Authors:  Divya Awasthi; Kunal Kumar; Iwao Ojima
Journal:  Expert Opin Ther Pat       Date:  2011-03-18       Impact factor: 6.674

5.  A 4-aminofurazan derivative-A189-inhibits assembly of bacterial cell division protein FtsZ in vitro and in vivo.

Authors:  Hideaki Ito; Atsushi Ura; Yoshihiro Oyamada; Akihiko Tanitame; Hiroaki Yoshida; Sakuo Yamada; Masaaki Wachi; Jun-ichi Yamagishi
Journal:  Microbiol Immunol       Date:  2006       Impact factor: 1.955

Review 6.  Therapeutic options for infections due to vancomycin-resistant enterococci.

Authors:  Jiun-Ling Wang; Po-Ren Hsueh
Journal:  Expert Opin Pharmacother       Date:  2009-04       Impact factor: 3.889

7.  A new 2-carbamoyl pteridine that inhibits mycobacterial FtsZ.

Authors:  R C Reynolds; S Srivastava; L J Ross; W J Suling; E L White
Journal:  Bioorg Med Chem Lett       Date:  2004-06-21       Impact factor: 2.823

8.  2-Alkoxycarbonylaminopyridines: inhibitors of Mycobacterium tuberculosis FtsZ.

Authors:  E Lucile White; William J Suling; Larry J Ross; Lainne E Seitz; Robert C Reynolds
Journal:  J Antimicrob Chemother       Date:  2002-07       Impact factor: 5.790

Review 9.  Streptomycin and alternative agents for the treatment of tularemia: review of the literature.

Authors:  G Enderlin; L Morales; R F Jacobs; J T Cross
Journal:  Clin Infect Dis       Date:  1994-07       Impact factor: 9.079

10.  Inhibition of bacterial cell division protein FtsZ by cinnamaldehyde.

Authors:  Prerna Domadia; Sanjay Swarup; Anirban Bhunia; J Sivaraman; Debjani Dasgupta
Journal:  Biochem Pharmacol       Date:  2007-06-23       Impact factor: 5.858
View more
  9 in total

1.  Glochidioboside Kills Pathogenic Bacteria by Membrane Perturbation.

Authors:  Heejeong Lee; Eun-Rhan Woo; Dong Gun Lee
Journal:  Curr Microbiol       Date:  2015-03-29       Impact factor: 2.188

2.  Synthesis and investigation of novel benzimidazole derivatives as antifungal agents.

Authors:  Nishad Thamban Chandrika; Sanjib K Shrestha; Huy X Ngo; Sylvie Garneau-Tsodikova
Journal:  Bioorg Med Chem       Date:  2016-06-04       Impact factor: 3.641

3.  Strategic incorporation of fluorine in the drug discovery of new-generation antitubercular agents targeting bacterial cell division protein FtsZ.

Authors:  Iwao Ojima; Divya Awasthi; Longfei Wei; Krupanandan Haranahalli
Journal:  J Fluor Chem       Date:  2016-07-29       Impact factor: 2.050

Review 4.  Recent advances in the discovery and development of antibacterial agents targeting the cell-division protein FtsZ.

Authors:  Krupanandan Haranahalli; Simon Tong; Iwao Ojima
Journal:  Bioorg Med Chem       Date:  2016-05-05       Impact factor: 3.641

5.  Bis-indolic compounds as potential new therapeutic alternatives for tularaemia.

Authors:  Yvan Caspar; Vivien Sutera; Sandrine Boisset; Jean-Noël Denis; Max Maurin
Journal:  Front Cell Infect Microbiol       Date:  2014-02-27       Impact factor: 5.293

6.  A trisubstituted benzimidazole cell division inhibitor with efficacy against Mycobacterium tuberculosis.

Authors:  Susan E Knudson; Divya Awasthi; Kunal Kumar; Alexandra Carreau; Laurent Goullieux; Sophie Lagrange; Hélèn Vermet; Iwao Ojima; Richard A Slayden
Journal:  PLoS One       Date:  2014-04-15       Impact factor: 3.240

Review 7.  Antimicrobial potential of 1H-benzo[d]imidazole scaffold: a review.

Authors:  Sumit Tahlan; Sanjiv Kumar; Balasubramanian Narasimhan
Journal:  BMC Chem       Date:  2019-02-04

8.  4-(2-(1H-Benzo[d]imidazol-2-ylthio)acetamido)-N-(substituted phenyl)benzamides: design, synthesis and biological evaluation.

Authors:  Sumit Tahlan; Kalavathy Ramasamy; Siong Meng Lim; Syed Adnan Ali Shah; Vasudevan Mani; Balasubramanian Narasimhan
Journal:  BMC Chem       Date:  2019-02-02

9.  TPR1, a novel rifampicin derivative, demonstrates efficacy alone and in combination with doxycycline against the NIAID Category A priority pathogen Francisella tularensis.

Authors:  Jason E Cummings; Keaton W Slayden; Richard A Slayden
Journal:  JAC Antimicrob Resist       Date:  2021-05-04
  9 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.