Increment of Antimycobaterial Activity on Lichexanthone Derivatives


Autoria(s): Micheletti, Ana Camila; Honda, Neli Kika; Pavan, Fernando Rogério; Leite, Clarice Queico Fujimura; Cepa Matos, Maria de Fatima; Perdomo, Renata Trentin; Bogo, Danielle; Alcantara, Glaucia Braz; Beatriz, Adilson
Contribuinte(s)

Universidade Estadual Paulista (UNESP)

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