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Boron-based drugs as antiprotozoals.
Jacobs, Robert T; Plattner, Jacob J; Keenan, Martine.
Affiliation
  • Jacobs RT; SCYNEXIS Inc., Research Triangle Park, North Carolina, USA. bob.jacobs@scynexis.com
Curr Opin Infect Dis ; 24(6): 586-92, 2011 Dec.
Article in En | MEDLINE | ID: mdl-22001943
ABSTRACT
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.
Subject(s)

Full text: 1 Database: MEDLINE Main subject: Trypanosomiasis, African / Boron Compounds / Chagas Disease / Malaria / Antiprotozoal Agents Type of study: Prognostic_studies Limits: Humans Language: En Year: 2011 Type: Article

Full text: 1 Database: MEDLINE Main subject: Trypanosomiasis, African / Boron Compounds / Chagas Disease / Malaria / Antiprotozoal Agents Type of study: Prognostic_studies Limits: Humans Language: En Year: 2011 Type: Article