1268085-01-3Relevant academic research and scientific papers
Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity
Kotb, Ahmed,Abutaleb, Nader S.,Seleem, Mohamed A.,Hagras, Mohamed,Mohammad, Haroon,Bayoumi, Ashraf,Ghiaty, Adel,Seleem, Mohamed N.,Mayhoub, Abdelrahman S.
, p. 110 - 120 (2018)
A new series of phenylthiazoles with t-butyl lipophilic component was synthesized and their antibacterial activity against a panel of multidrug-resistant bacterial pathogens was evaluated. Five compounds demonstrated promising antibacterial activity against methicillin-resistant staphylococcal strains and several vancomycin-resistant staphylococcal and enterococcal species. Additionally, three derivatives 19, 23 and 26 exhibited rapid bactericidal activity, and remarkable ability to disrupt mature biofilm produced by MRSA USA300. More importantly, a resistant mutant to 19 couldn't be isolated after subjecting MRSA to sub-lethal doses for 14 days. Lastly, this new series of phenylthiazoles possesses an advantageous attribute over the first-generation compounds in their stability to hepatic metabolism, with a biological half-life of more than 9 h.
PHENYLTHIAZOLES AND USES THEREOF
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Paragraph 0085, (2018/11/24)
Series of 2-phenyl-4-methylthiazole analogues are disclosed as potential therapeutic agents for the treatment of bacterial infections, especially methicillin-resistant Straphylococcus aureus (MRSA) related infections. A method for the treatment of MRSA-re
ANTIMICROBIAL SUBSTITUTED THIAZOLES AND METHODS OF USE
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Paragraph 0051; 0056, (2014/05/08)
Disclosed are compositions having activity against MRSA and/or VRSA, and methods of using the compositions to treat microbial infections.
Discovery and characterization of potent thiazoles versus methicillin- and vancomycin-resistant Staphylococcus aureus
Mohammad, Haroon,Mayhoub, Abdelrahman S.,Ghafoor, Adil,Soofi, Muhammad,Alajlouni, Ruba A.,Cushman, Mark,Seleem, Mohamed N.
, p. 1609 - 1615 (2014/03/21)
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.
