Evaluation of the Structure-Activity Relationship of Rifabutin and Analogs: A Drug-Membrane Study

• Tipo: Artigo em Revista Científica Internacional
• Data: 2013

Autores

Marina Pinheiro (Autor) Outra; Catarina Pereira Leite (Autor) Outra; Mariana Arede (Autor) Outra; Claudia Nunes (Autor) Outra; Joao M Caio (Autor) Outra; Cristina Moiteiro (Autor) Outra; Juan J Giner Casares (Autor) Outra; Marlene Lucio (Autor) FFUP; Gerald Brezesinski (Autor) Outra; Luis Camacho (Autor) Outra; Salette Reis (Autor) FFUP

Revista

Título: ChemPhysChem

Vol. 14

Páginas: 2808-2816

ISSN: 1439-4235

Editora: Wiley-Blackwell

Indexação

ISI Web of Knowledge - 8 Citações

Scopus - 11 Citações

Classificação Científica

FOS: Ciências exactas e naturais > Química

Outras Informações

ID Authenticus: P-006-85H

DOI: 10.1002/cphc.201300262

Abstract (EN): 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.

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 9