Design, characterization, in vitro antibacterial, antitubercular evaluation and structure–activity relationships of new hydrazinyl thiazolyl coumarin derivatives
Herein, we describe the synthesis of 11new thiazolyl coumarin derivatives and evaluation of their potential role as antibacterial and antituberculosis agents. The structures of the synthesized compounds were established by extensive spectroscopic studies (Fourier transform infrared spectroscopy, 1H-...
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my.ums.eprints.193442018-03-22T02:14:22Z https://eprints.ums.edu.my/id/eprint/19344/ Design, characterization, in vitro antibacterial, antitubercular evaluation and structure–activity relationships of new hydrazinyl thiazolyl coumarin derivatives Samina KhanYusufzai Hasnah Osman Mohammad Shaheen Khan Suriyati Mohamad Othman Sulaiman Thaigarajan Parumasivam Azlan Jualang Gansau Norhaniza Johansah Noviany RC Internal medicine Herein, we describe the synthesis of 11new thiazolyl coumarin derivatives and evaluation of their potential role as antibacterial and antituberculosis agents. The structures of the synthesized compounds were established by extensive spectroscopic studies (Fourier transform infrared spectroscopy, 1H-nuclear magnetic resonance, 13C-nuclear magnetic resonance, 2D-nuclear magnetic resonance and liquid chromatography–mass spectrometry) and elemental analysis. All synthesized compounds were assayed for their in vitro antibacterial activity against a few gram positive and gram negative bacteria and antituberculosis activity against Mycobacterium tuberculosis H37Rv ATCC 25618 by using colorimetric microdilution assay method. Nine derivatives showed moderate anti-bacterial and anti-tuberculosis activities against all the tested strains. The highest activity against all the pathogens including Mycobacterium tuberculosis was observed by compound 7c with MIC values ranging between 31.25–62.5 μg/mL, indicating that coumarin skeleton could indeed provide useful scaffold for the development of new anti-microbial drugs. Springer US 2017-06 Article PeerReviewed text en https://eprints.ums.edu.my/id/eprint/19344/1/Design.pdf Samina KhanYusufzai and Hasnah Osman and Mohammad Shaheen Khan and Suriyati Mohamad and Othman Sulaiman and Thaigarajan Parumasivam and Azlan Jualang Gansau and Norhaniza Johansah and Noviany (2017) Design, characterization, in vitro antibacterial, antitubercular evaluation and structure–activity relationships of new hydrazinyl thiazolyl coumarin derivatives. Medicinal Chemistry Research, 26 (6). pp. 1139-1148. ISSN 1554-8120 https://doi.org/10.1007/s00044-017-1820-2 |
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RC Internal medicine Samina KhanYusufzai Hasnah Osman Mohammad Shaheen Khan Suriyati Mohamad Othman Sulaiman Thaigarajan Parumasivam Azlan Jualang Gansau Norhaniza Johansah Noviany Design, characterization, in vitro antibacterial, antitubercular evaluation and structure–activity relationships of new hydrazinyl thiazolyl coumarin derivatives |
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Herein, we describe the synthesis of 11new thiazolyl coumarin derivatives and evaluation of their potential role as antibacterial and antituberculosis agents. The structures of the synthesized compounds were established by extensive spectroscopic studies (Fourier transform infrared spectroscopy, 1H-nuclear magnetic resonance, 13C-nuclear magnetic resonance, 2D-nuclear magnetic resonance and liquid chromatography–mass spectrometry) and elemental analysis. All synthesized compounds were assayed for their in vitro antibacterial activity against a few gram positive and gram negative bacteria and antituberculosis activity against Mycobacterium tuberculosis H37Rv ATCC 25618 by using colorimetric microdilution assay method. Nine derivatives showed moderate anti-bacterial and anti-tuberculosis activities against all the tested strains. The highest activity against all the pathogens including Mycobacterium tuberculosis was observed by compound 7c with MIC values ranging between 31.25–62.5 μg/mL, indicating that coumarin skeleton could indeed provide useful scaffold for the development of new anti-microbial drugs. |
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Article |
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Samina KhanYusufzai Hasnah Osman Mohammad Shaheen Khan Suriyati Mohamad Othman Sulaiman Thaigarajan Parumasivam Azlan Jualang Gansau Norhaniza Johansah Noviany |
author_facet |
Samina KhanYusufzai Hasnah Osman Mohammad Shaheen Khan Suriyati Mohamad Othman Sulaiman Thaigarajan Parumasivam Azlan Jualang Gansau Norhaniza Johansah Noviany |
author_sort |
Samina KhanYusufzai |
title |
Design, characterization, in vitro antibacterial, antitubercular evaluation and structure–activity relationships of new hydrazinyl thiazolyl coumarin derivatives |
title_short |
Design, characterization, in vitro antibacterial, antitubercular evaluation and structure–activity relationships of new hydrazinyl thiazolyl coumarin derivatives |
title_full |
Design, characterization, in vitro antibacterial, antitubercular evaluation and structure–activity relationships of new hydrazinyl thiazolyl coumarin derivatives |
title_fullStr |
Design, characterization, in vitro antibacterial, antitubercular evaluation and structure–activity relationships of new hydrazinyl thiazolyl coumarin derivatives |
title_full_unstemmed |
Design, characterization, in vitro antibacterial, antitubercular evaluation and structure–activity relationships of new hydrazinyl thiazolyl coumarin derivatives |
title_sort |
design, characterization, in vitro antibacterial, antitubercular evaluation and structure–activity relationships of new hydrazinyl thiazolyl coumarin derivatives |
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Springer US |
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2017 |
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https://eprints.ums.edu.my/id/eprint/19344/1/Design.pdf https://eprints.ums.edu.my/id/eprint/19344/ https://doi.org/10.1007/s00044-017-1820-2 |
_version_ |
1760229568188252160 |
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13.1890135 |