Increment of Antimycobaterial Activity on Lichexanthone Derivatives

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]

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

• 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
• Modalidade de apoio: 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
• Modalidade de apoio: Bolsas no Brasil - Doutorado