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Issue 2, 2015
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4-Thiazolidinone derivatives as potent antimicrobial agents: microwave-assisted synthesis, biological evaluation and docking studies

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Abstract

As a part of our ongoing research in the development of new antimicrobials, herein, we report the synthesis of ten compounds which combine three bioactive moieties: thiazole, adamantane and 4-thiazolidinone. Evaluation of their antibacterial activity revealed that the newly synthesized compounds exhibited remarkable growth inhibition of a wide spectrum of Gram-positive bacteria, Gram-negative bacteria and fungi. The majority of the compounds displayed greater antibacterial activity than the reference drugs (ampicillin and streptomycin), while the antifungal activity was significantly higher than that of the reference drugs bifonazole and ketoconazole. Additionally, the title compounds were screened for HIV-1 reverse transcriptase inhibitory activity, showing no significant activity. Moreover, docking studies were performed in order to explore possible binding modes at the MurB protein of S. aureus.

Graphical abstract: 4-Thiazolidinone derivatives as potent antimicrobial agents: microwave-assisted synthesis, biological evaluation and docking studies

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Publication details

The article was received on 11 Sep 2014, accepted on 31 Oct 2014 and first published on 19 Nov 2014


Article type: Concise Article
DOI: 10.1039/C4MD00399C
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Med. Chem. Commun., 2015,6, 319-326

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    4-Thiazolidinone derivatives as potent antimicrobial agents: microwave-assisted synthesis, biological evaluation and docking studies

    E. Pitta, E. Tsolaki, A. Geronikaki, J. Petrović, J. Glamočlija, M. Soković, E. Crespan, G. Maga, S. S. Bhunia and A. K. Saxena, Med. Chem. Commun., 2015, 6, 319
    DOI: 10.1039/C4MD00399C

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