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.
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.
Authors: Katrien Van Bocxlaer; Eric Gaukel; Deirdre Hauser; Seong Hee Park; Sara Schock; Vanessa Yardley; Ryan Randolph; Jacob J Plattner; Tejal Merchant; Simon L Croft; Robert T Jacobs; Stephen A Wring Journal: Antimicrob Agents Chemother Date: 2018-04-26 Impact factor: 5.191
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Authors: Suman K Vodnala; Thomas Lundbäck; Birger Sjöberg; Richard Svensson; Martin E Rottenberg; Lars G J Hammarström Journal: Antimicrob Agents Chemother Date: 2012-12-17 Impact factor: 5.191
Authors: Ebere Sonoiki; Caroline L Ng; Marcus C S Lee; Denghui Guo; Yong-Kang Zhang; Yasheen Zhou; M R K Alley; Vida Ahyong; Laura M Sanz; Maria Jose Lafuente-Monasterio; Chen Dong; Patrick G Schupp; Jiri Gut; Jenny Legac; Roland A Cooper; Francisco-Javier Gamo; Joseph DeRisi; Yvonne R Freund; David A Fidock; Philip J Rosenthal Journal: Nat Commun Date: 2017-03-06 Impact factor: 14.919
Authors: Maureen Gumbo; Richard M Beteck; Tawanda Mandizvo; Ronnett Seldon; Digby F Warner; Heinrich C Hoppe; Michelle Isaacs; Dustin Laming; Christina C Tam; Luisa W Cheng; Nicole Liu; Kirkwood M Land; Setshaba D Khanye Journal: Molecules Date: 2018-08-15 Impact factor: 4.411