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Please use this identifier to cite or link to this item: http://repository.li.mahidol.ac.th/dspace/handle/123456789/33671
Title: Antimycobacterial activity of natural products and synthetic agents: Pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis
Authors: Dakshina U. Ganihigama
Sanya Sureram
Sasithorn Sangher
Poonpilas Hongmanee
Thammarat Aree
Chulabhorn Mahidol
Somsak Ruchirawat
Prasat Kittakoop
Chulabhorn Graduate Institute
Chulabhorn Research Institute
Mahidol University
Chulalongkorn University
South Carolina Commission on Higher Education
Keywords: Chemistry;Pharmacology, Toxicology and Pharmaceutics
Issue Date: 1-Jan-2014
Citation: European Journal of Medicinal Chemistry. Vol.89, (2014), 1-12
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.
URI: https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84908405187&origin=inward
http://repository.li.mahidol.ac.th/dspace/handle/123456789/33671
ISSN: 17683254
02235234
Appears in Collections:Scopus 2011-2015

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