Literature DB >> 24387054

Discovery and characterization of potent thiazoles versus methicillin- and vancomycin-resistant Staphylococcus aureus.

Haroon Mohammad1, Abdelrahman S Mayhoub, Adil Ghafoor, Muhammad Soofi, Ruba A Alajlouni, Mark Cushman, Mohamed N Seleem.   

Abstract

Methicillin- and vancomycin-resistant Staphylococcus aureus (MRSA and VRSA) infections are growing global health concerns. Structure-activity relationships of phenylthiazoles as a new antimicrobial class have been addressed. We present 10 thiazole derivatives that exhibit strong activity against 18 clinical strains of MRSA and VRSA with acceptable PK profile. Three derivatives revealed an advantage over vancomycin by rapidly eliminating MRSA growth within 6 h, and no derivatives are toxic to HeLa cells at 11 μg/mL.

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Year:  2014        PMID： 24387054      PMCID： PMC4353699          DOI： 10.1021/jm401905m

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  14 in total

1.  Antitumour benzothiazoles. Part 20: 3'-cyano and 3'-alkynyl-substituted 2-(4'-aminophenyl)benzothiazoles as new potent and selective analogues.

Authors:  Ian Hutchinson; Tracey D Bradshaw; Charles S Matthews; Malcolm F G Stevens; Andrew D Westwell
Journal:  Bioorg Med Chem Lett       Date:  2003-02-10       Impact factor: 2.823

2.  Linezolid resistance in clinical isolates of Staphylococcus aureus.

Authors:  Peter Wilson; J A Andrews; R Charlesworth; R Walesby; M Singer; D J Farrell; M Robbins
Journal:  J Antimicrob Chemother       Date:  2003-01       Impact factor: 5.790

3.  Methicillin-resistant S. aureus infections among patients in the emergency department.

Authors:  Gregory J Moran; Anusha Krishnadasan; Rachel J Gorwitz; Gregory E Fosheim; Linda K McDougal; Roberta B Carey; David A Talan
Journal:  N Engl J Med       Date:  2006-08-17       Impact factor: 91.245

4.  An investigation of phenylthiazole antiflaviviral agents.

Authors:  Abdelrahman S Mayhoub; Mansoora Khaliq; Carolyn Botting; Ze Li; Richard J Kuhn; Mark Cushman
Journal:  Bioorg Med Chem       Date:  2011-05-03       Impact factor: 3.641

5.  Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56(lck) inhibitors.

Authors:  Jagabandhu Das; Robert V Moquin; James Lin; Chunjian Liu; Arthur M Doweyko; Henry F DeFex; Qiong Fang; Suhong Pang; Sidney Pitt; Ding Ren Shen; Gary L Schieven; Joel C Barrish; John Wityak
Journal:  Bioorg Med Chem Lett       Date:  2003-08-04       Impact factor: 2.823

Review 6.  Antibiotics for emerging pathogens.

Authors:  Michael A Fischbach; Christopher T Walsh
Journal:  Science       Date:  2009-08-28       Impact factor: 47.728

7.  In vitro 24-hour time-kill studies of vancomycin and linezolid in combination versus methicillin-resistant Staphylococcus aureus.

Authors:  Shveta Rani Singh; Alfred E Bacon; David C Young; Kimberly A Couch
Journal:  Antimicrob Agents Chemother       Date:  2009-07-27       Impact factor: 5.191

8.  Synthesis and pharmacological evaluation of a novel series of 3-aryl-2-(2-substituted-4-methylthiazole-5-yl)thiazolidin-4-one as possible anti-inflammatory and antimicrobial agents.

Authors:  Shivaji H Shelke; Pravin C Mhaske; Mukesh Nandave; Sachin Narkhade; Namdeo M Walhekar; Vivek D Bobade
Journal:  Bioorg Med Chem Lett       Date:  2012-08-25       Impact factor: 2.823

Review 9.  Vancomycin in combination with other antibiotics for the treatment of serious methicillin-resistant Staphylococcus aureus infections.

Authors:  Stan Deresinski
Journal:  Clin Infect Dis       Date:  2009-10-01       Impact factor: 9.079

10.  Skin and soft tissue infections caused by methicillin-resistant Staphylococcus aureus USA300 clone.

Authors:  Jennifer K Johnson; Tina Khoie; Simone Shurland; Kristen Kreisel; O Colin Stine; Mary-Claire Roghmann
Journal:  Emerg Infect Dis       Date:  2007-08       Impact factor: 6.883
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  21 in total

1.  Discovery and Development of 8-Substituted Cycloberberine Derivatives as Novel Antibacterial Agents against MRSA.

Authors:  Tianyun Fan; Xinxin Hu; Sheng Tang; Xiaojia Liu; Yanxiang Wang; Hongbin Deng; Xuefu You; Jiandong Jiang; Yinghong Li; Danqing Song
Journal:  ACS Med Chem Lett       Date:  2018-04-16       Impact factor: 4.345

2.  Arylthiazole antibiotics targeting intracellular methicillin-resistant Staphylococcus aureus (MRSA) that interfere with bacterial cell wall synthesis.

Authors:  Islam Eid; Mohamed M Elsebaei; Haroon Mohammad; Mohamed Hagras; Christine E Peters; Youssef A Hegazy; Bruce Cooper; Joe Pogliano; Kit Pogliano; Hamada S Abulkhair; Mohamed N Seleem; Abdelrahman S Mayhoub
Journal:  Eur J Med Chem       Date:  2017-08-18       Impact factor: 6.514

3.  Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.

Authors:  Mohamed Hagras; Youssef A Hegazy; Amr H Elkabbany; Haroon Mohammad; Adel Ghiaty; Tamer M Abdelghany; Mohamed N Seleem; Abdelrahman S Mayhoub
Journal:  Eur J Med Chem       Date:  2017-10-19       Impact factor: 6.514

4.  Phenylthiazole Antibacterial Agents Targeting Cell Wall Synthesis Exhibit Potent Activity in Vitro and in Vivo against Vancomycin-Resistant Enterococci.

Authors:  Haroon Mohammad; Waleed Younis; Lu Chen; Christine E Peters; Joe Pogliano; Kit Pogliano; Bruce Cooper; Jianan Zhang; Abdelrahman Mayhoub; Eric Oldfield; Mark Cushman; Mohamed N Seleem
Journal:  J Med Chem       Date:  2017-03-15       Impact factor: 7.446

5.  An aryl isonitrile compound with an improved physicochemical profile that is effective in two mouse models of multidrug-resistant Staphylococcus aureus infection.

Authors:  Haroon Mohammad; Kwaku Kyei-Baffour; Nader S Abutaleb; Mingji Dai; Mohamed N Seleem
Journal:  J Glob Antimicrob Resist       Date:  2019-04-30       Impact factor: 4.035

6.  Discovery of a Novel Dibromoquinoline Compound Exhibiting Potent Antifungal and Antivirulence Activity That Targets Metal Ion Homeostasis.

Authors:  Haroon Mohammad; Nehal H Elghazawy; Hassan E Eldesouky; Youssef A Hegazy; Waleed Younis; Larisa Avrimova; Tony Hazbun; Reem K Arafa; Mohamed N Seleem
Journal:  ACS Infect Dis       Date:  2018-02-02       Impact factor: 5.084

7.  Anti-biofilm activity and synergism of novel thiazole compounds with glycopeptide antibiotics against multidrug-resistant staphylococci.

Authors:  Haroon Mohammad; Abdelrahman S Mayhoub; Mark Cushman; Mohamed N Seleem
Journal:  J Antibiot (Tokyo)       Date:  2014-10-15       Impact factor: 2.649

Review 8.  Thiazole Ring-A Biologically Active Scaffold.

Authors:  Anthi Petrou; Maria Fesatidou; Athina Geronikaki
Journal:  Molecules       Date:  2021-05-25       Impact factor: 4.411

9.  Alkynyl-containing phenylthiazoles: Systemically active antibacterial agents effective against methicillin-resistant Staphylococcus aureus (MRSA).

Authors:  Mohamed M Elsebaei; Haroon Mohammad; Mohamed Abouf; Nader S Abutaleb; Youssef A Hegazy; Adel Ghiaty; Lu Chen; Jianan Zhang; Satish R Malwal; Eric Oldfield; Mohamed N Seleem; Abdelrahman S Mayhoub
Journal:  Eur J Med Chem       Date:  2018-02-12       Impact factor: 6.514

10.  Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.

Authors:  Ahmed Kotb; Nader S Abutaleb; Mohamed A Seleem; Mohamed Hagras; Haroon Mohammad; Ashraf Bayoumi; Adel Ghiaty; Mohamed N Seleem; Abdelrahman S Mayhoub
Journal:  Eur J Med Chem       Date:  2018-03-19       Impact factor: 6.514
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