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(Referência obtida automaticamente do Web of Science, por meio da informação sobre o financiamento pela FAPESP e o número do processo correspondente, incluída na publicação pelos autores.)

Increment of Antimycobaterial Activity on Lichexanthone Derivatives

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Autor(es):
Micheletti, Ana Camila [1] ; Honda, Neli Kika [1] ; Pavan, Fernando R. [2] ; Leite, Clarice Q. F. [2] ; Cepa Matos, Maria de Fatima [3] ; Perdomo, Renata Trentin [3] ; Bogo, Danielle [3] ; Alcantara, Glaucia Braz [1] ; Beatriz, Adilson [1]
Número total de Autores: 9
Afiliação do(s) autor(es):
[1] Univ Fed Mato Grosso do Sul, Ctr Ciencias Exatas & Tecnol, Campo Grande, MS - Brazil
[2] Univ Estadual Paulista, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP - Brazil
[3] Univ Fed Mato Grosso do Sul, Ctr Ciencias Biol & Saude, Campo Grande, MS - Brazil
Número total de Afiliações: 3
Tipo de documento: Artigo Científico
Fonte: Medicinal Chemistry; v. 9, n. 7, p. 904-910, NOV 2013.
Citações Web of Science: 4
Resumo

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. (AU)

Processo FAPESP: 09/06499-1 - Determinação da atividade anti-tuberculose in vitro e in vivo de complexos de Ru(II) fosfinas/diiminas
Beneficiário:Clarice Queico Fujimura Leite
Linha de fomento: Auxílio à Pesquisa - Regular
Processo FAPESP: 08/10390-2 - Determinação do perfil pré-clínico da atividade antituberculose in vitro e in vivo dos complexos de rutênio(II)fosfinas / diiminas
Beneficiário:Fernando Rogério Pavan
Linha de fomento: Bolsas no Brasil - Doutorado