Application of enzyme prodrugs as anti-infective agents

Chemistry: molecular biology and microbiology – Measuring or testing process involving enzymes or... – Involving viable micro-organism

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435 30, 435 43, 435 6, 435 2, 424 91, 530300, 530335, 514 16, 514 18, 514199, 514206, 514204, 514203, 514246, 540222, 540225, C12Q 118, C12Q 126, C07D 500, A61K 3800, A61K 3143

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061597066

ABSTRACT:
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.

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