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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Increment of Antimycobaterial Activity on Lichexanthone Derivatives

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Author(s):
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]
Total Authors: 9
Affiliation:
[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
Total Affiliations: 3
Document type: Journal article
Source: Medicinal Chemistry; v. 9, n. 7, p. 904-910, NOV 2013.
Web of Science Citations: 4
Abstract

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)

FAPESP's process: 09/06499-1 - Determination of in vitro and in vivo anti-tuberculosis activity of phosphines/diimines Ru (II) complexes
Grantee:Clarice Queico Fujimura Leite
Support Opportunities: Regular Research Grants
FAPESP's process: 08/10390-2 - Determination of pre-clinical profile in vitro and in vivo anti-tuberculosis activity of ruthenium(II)phosphine / picolinate complexes
Grantee:Fernando Rogério Pavan
Support Opportunities: Scholarships in Brazil - Doctorate