Increment of Antimycobaterial Activity on Lichexanthone Derivatives
Contribuinte(s) |
Universidade Estadual Paulista (UNESP) |
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Data(s) |
03/12/2014
03/12/2014
01/11/2013
|
Resumo |
Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) Processo FAPESP: 08/10390-2 Processo FAPESP: 09/06499-1 A new dihydropyranexanthone derived from the natural xanthone lichexanthone (1) was synthesised and, together with other 18 derivatives including omega-bromo and omega-aminoalkoxylxanthones (containing methyl, ethyl, propyl, tert-butylamino and piperidinyl moieties), were tested against Mycobacterium tuberculosis. Nine omega-aminoalkoxylxanthones showed good antimycobacterial activity, and their in vitro cytotoxicity was determined using VERO cells in order to calculate the selectivity index (SI). One of these nitrogenated xanthone derivatives showed very promising results, with MIC of 2.6 mu M and SI of 48. This MIC is comparable to values found in first and second line drugs commonly used to treat TB. In order to understand better about this compound, it was evaluated together with two other ones that showed good SI, against resistant clinical strains of M. tuberculosis to verify the existence of cross-resistance. A chemometrical approach was useful to establish a pattern of antitubercular activity among the group of -aminoalkoxylxanthones, according to some structural and chemical features. |
Formato |
904-910 |
Identificador |
http://dx.doi.org/10.2174/1573406411309070003 Medicinal Chemistry. Sharjah: Bentham Science Publ Ltd, v. 9, n. 7, p. 904-910, 2013. 1573-4064 http://hdl.handle.net/11449/112072 WOS:000326089300002 |
Idioma(s) |
eng |
Publicador |
Bentham Science Publ Ltd |
Relação |
Medicinal Chemistry |
Direitos |
closedAccess |
Palavras-Chave | #Chemometrics #lichen #structural modifications #tuberculosis #xanthone |
Tipo |
info:eu-repo/semantics/article |