Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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3-(1-Adamantylthio)-4-Phenylpyridine as a Potential Therapeutic for Methicillin-Resistant Staphylococcus aureus

Author(s): Ratana Lawung, Lertyot Treeratanapiboon, Supaluk Prachayasittikul, Virapong Prachayasittikul.

Abstract:

In a previous study, 5-(1-adamantylthio)-3-picoline (I) and 3-(1-adamantylthio)-4-phenylpyridine (II) were shown to have potent antimicrobial activity. The present investigation is concerned with the antimicrobial action of thiopyridines I and II against methicillin-resistant Staphylococcus aureus (MRSA) isolates and with their murine fibroblast (L929) cytotoxicity. Thiopyridine II was found to display significant antimicrobial activity against all of the MRSA isolates tested, with minimum inhibitory concentrations (MIC) of 1-8 μg/mL. Moreover, both I and II attenuate the viability of L929 cells in a dose-dependent manner, displaying an IC50 of 68.4±6.0 and 47.3±5.6 μg/mL, respectively. These findings suggest that thiopyridine II is promising as a lead compound for further development as a therapeutic.

Keywords: 3-(1-Adamantylthio)-4-phenylpyridine, Methicillin resistant Staphylococcus aureus, MTT assay, Antimicrobial activity, Susceptibility testing, Potential Therapeutic, Methicillin resistant Staphylococcu aureus, Penicillin-resistant, Streptococcus pneumoniae (PRSP), Vancomycin-resistant enterococci (VRE), Community-acquired infections, Penicillins, Cephalosphorins, Carbapenems, Aminoglycosides, Tetracyclines, Chloramphenicol and quinolones, Gene-regulator function, Multi-drug-resistant, Cytotoxic effects, Methicillin-resistant, Pneumonia, Skin infection, Gentamiein, Erythromycin, Clindamycin, Lactams, Gentamicin, Gentamieih, Trimethoprim-sulfamethoxazole, Cell line, Culture medium, Growth inhibition, Cytotoxicity test, % Cell viability, Linezolid, Ceftobiprole, Daptomycin, Tigecycline, Thiopyridine, Antibiotic-resistant bacteria, Nosocomial pneumonia, Serotonin toxicity

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Article Details

VOLUME: 7
ISSUE: 9
Year: 2010
Page: [674 - 678]
Pages: 5
DOI: 10.2174/157018010792929603
Price: $58