Publication: Antimycobacterial activity of natural products and synthetic agents: Pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis
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Issued Date
2014-01-01
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ISSN
17683254
02235234
02235234
Other identifier(s)
2-s2.0-84908405187
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Mahidol University
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SCOPUS
Bibliographic Citation
European Journal of Medicinal Chemistry. Vol.89, (2014), 1-12
Suggested Citation
Dakshina U. Ganihigama, Sanya Sureram, Sasithorn Sangher, Poonpilas Hongmanee, Thammarat Aree, Chulabhorn Mahidol, Somsak Ruchirawat, Prasat Kittakoop Antimycobacterial activity of natural products and synthetic agents: Pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis. European Journal of Medicinal Chemistry. Vol.89, (2014), 1-12. doi:10.1016/j.ejmech.2014.10.026 Retrieved from: https://repository.li.mahidol.ac.th/handle/123456789/33671
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Title
Antimycobacterial activity of natural products and synthetic agents: Pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis
Abstract
© 2014 Elsevier Masson SAS. All rights reserved. Various classes of natural products and synthetic compounds were tested against reference strains and clinical multidrug resistant isolates of Mycobacterium tuberculosis. Vermelhotin (19), a natural tetramic acid from fungi, was the most active toward clinical MDR TB isolates (MIC 1.5-12.5 μg/mL). Synthetic compounds (i.e. benzoxazocines, coumarins, chromenes, and pyrrolodiquinoline derivatives) were prepared by green chemistry approaches. Under microwave irradiation, a one-pot synthesis of pyrrolodiquinoline 85 was achieved by homocoupling of 1-methylquinolinium iodide; the structure of 85 was confirmed by single-crystal X-ray analysis. Compound 85 and its derivative 86 exhibited potent antitubercular activity (MIC 0.3-6.2 μg/mL) against clinical MDR TB isolates, and they displayed weak cytotoxicity toward normal cell line. The scaffold of 85 and 86 is potential for antimycobacterial activity.