4.3 Review

Boron-based drugs as antiprotozoals

Journal

CURRENT OPINION IN INFECTIOUS DISEASES
Volume 24, Issue 6, Pages 586-592

Publisher

LIPPINCOTT WILLIAMS & WILKINS
DOI: 10.1097/QCO.0b013e32834c630e

Keywords

benzoxaboroles; Chagas disease; human African trypanosomiasis; malaria; neglected tropical diseases

Funding

  1. Drugs for Neglected Diseases initiative
  2. Medicines for Malaria Venture

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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 boroncontaining 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.

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