Publication Type Journal Article
Title Evaluation of the Structure-Activity Relationship of Rifabutin and Analogs: A Drug-Membrane Study
Authors Marina Pinheiro Catarina Pereira-Leite Mariana Arede Claudia Nunes Joao Caio C. M. M. Moiteiro Juan J. Giner-Casares Marlene Lucio Gerald Brezesinski Luis Camacho Salette Reis
Groups HC
Journal CHEMPHYSCHEM
Year 2013
Month August
Volume 14
Number 12
Pages 2808-2816
Abstract This work focuses on the influence of rifabutin and two novel analogs, namely, N-acetyl-rifabutin and N-butanoyl-rifabutin, on the biophysical properties of lipid membranes. Monolayers and multilamellar vesicles composed of egg L—phosphatidylcholine:cholesterol in a molar ratio of 4:1 are chosen to mimic biological membranes. Several accurate biophysical techniques are used to establish a putative relationship between the chemical structure of the antimycobacterial compounds and their activity on the membranes. A combination of in situ experimental techniques, such as Langmuir isotherms, Brewster angle microscopy, polarization-modulated infrared reflection-absorption spectroscopy, and small-angle X-ray scattering, is used to assess the drug-membrane interaction. A relationship between the effect of a drug on the organization of the membranes and their chemical structure is found and may be useful in the development of new drugs with higher efficacy and fewer toxic effects.
DOI http://dx.doi.org/10.1002/cphc.201300262
ISBN
Publisher
Book Title
ISSN 1439-4235
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Conference Name
Bibtex ID ISI:000323196300030
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