Current opinion in infectious diseases · 2011
Boron-based drugs as antiprotozoals.
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Jacobs Robert T, Plattner Jacob J, Keenan Martine
Аннотация
PURPOSE OF REVIEW: Boron-based drugs represent a new class of molecules that have been found to exhibit attractive properties and activities against a number of protozoans causative of neglected tropical diseases.
RECENT FINDINGS: This review highlights recent advances in discovery of potential treatments for human African trypanosomiasis, malaria and Chagas disease from a class of boron-containing drugs, the benzoxaboroles.
SUMMARY: Research at several biotechnology companies, sponsored by product development partners (PDPs), has been successful in identifying a novel class of boron-based drugs, the benzoxaboroles, as potential treatments for neglected tropical diseases. This work was based, in part, on the earlier observation of antifungal, antibacterial and anti-inflammatory activities of the benzoxaboroles. The unique properties of boron, namely its ability to reversibly interact with biochemical targets through an empty p-orbital, are important to the success of these new drug candidates. Physicochemical and pharmacokinetic properties of the boron-based compounds are consistent with features required for oral absorption, metabolic stability and low toxicity - all important for progression of this class to clinical trials.
RECENT FINDINGS: This review highlights recent advances in discovery of potential treatments for human African trypanosomiasis, malaria and Chagas disease from a class of boron-containing drugs, the benzoxaboroles.
SUMMARY: Research at several biotechnology companies, sponsored by product development partners (PDPs), has been successful in identifying a novel class of boron-based drugs, the benzoxaboroles, as potential treatments for neglected tropical diseases. This work was based, in part, on the earlier observation of antifungal, antibacterial and anti-inflammatory activities of the benzoxaboroles. The unique properties of boron, namely its ability to reversibly interact with biochemical targets through an empty p-orbital, are important to the success of these new drug candidates. Physicochemical and pharmacokinetic properties of the boron-based compounds are consistent with features required for oral absorption, metabolic stability and low toxicity - all important for progression of this class to clinical trials.