Application of enzyme prodrugs as anti-infective agents

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 501/18 (2006.01) A61K 31/545 (2006.01) A61P 31/04 (2006.01) C12Q 1/18 (2006.01) G01N 33/573 (2006.01)

Patent

CA 2315201

The present invention provides a method for targeting toxic antimetabolites to gram negative infections. It provides a means of taking advantage of a key disease resistance mechanism to activate these drugs locally, and to overcome the resistance phenotype of the microbes. The invention further provides a method for selecting for antibiotic sensitivity, since a likely mechanism by which organisms are likely to gain resistance to the prodrugs is via loss of enzyme activity, which will make the bacteria sensitive to antibiotics once again.

La présente invention concerne une méthode permettant de cibler des antimétabolites toxiques sur des infections gram-négatives. Cette méthode s'appuie notamment sur un mécanisme de résistance aux maladies pour activer ces médicaments localement et vaincre le phénotype de résistance des microbes. L'invention concerne également une méthode d'étude de la sensibilité aux antibiotiques, l'un des mécanismes par lequel les organismes sont susceptibles d'améliorer leur résistance aux promédicaments reposant sur la perte de l'activité enzymatique, qui rend les bactéries à nouveau sensibles aux antibiotiques.

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