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Synthesis and antimycobacterial activity of 7-O-substituted-4-methyl-2H-2-chromenone derivativesvsMycobacterium tuberculosis

Yee, Sook Wah, Shah, Binal and Simons, Claire 2005. Synthesis and antimycobacterial activity of 7-O-substituted-4-methyl-2H-2-chromenone derivativesvsMycobacterium tuberculosis. Journal of Enzyme Inhibition and Medicinal Chemistry 20 (2) , pp. 109-113. 10.1080/14756360400002015

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Abstract

A series of 7-O-alkoxy-4-methylumbelliferone derivatives were prepared using a convenient one step synthesis. Additionally the bromo- and azido derivatives 7-O-(4-bromobutoxy)-, 7-O-(6-bromohexyloxy)- and 7-O-(6-azidohexyloxy)-4-methylumbelliferone derivatives were prepared. In vitro evaluation of antimycobacterial activity determined % inhibition and MIC vs M. tuberculosis H37Rv with toxicity (IC50) assessed in VERO cells. The coumarins with longer alkyl chains (nonyl and decyl) showed the optimum inhibitory activity in this series (MIC 3.13 μg/mL) and IC50>10 μg/mL.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Subjects: R Medicine > RS Pharmacy and materia medica
Uncontrolled Keywords: 7-O-alkyl-4-methylumbelliferone, antimycobacterial activity, MIC, toxicity (IC50)
Publisher: Informa Healthcare
ISSN: 1475-6374
Last Modified: 04 Jun 2017 02:56
URI: http://orca-mwe.cf.ac.uk/id/eprint/14004

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