Synthesis and in vitro protozoocidal activity of diazabicyclic benzotropolone derivatives.
We describe the synthesis and protozoocidal evaluation of a series of diazabicycles based on benzotropolone ethers. Several of the compounds, which can be obtained through a high-yielding hetero Diels-Alder reaction using simple and readily available starting materials, have in vitro activities against Trypanosoma cruzi and Leishmania donovani that are comparable to, and in some cases better than, those of currently used chemotherapies.
Khrizman
Alexander
A
Department of Chemistry & Biochemistry, University of the Sciences in Philadelphia, 600 South 43rd Street, Philadelphia, PA 19104-4495, USA.
Moulthrop
Jason S
JS
Little
Susan
S
Wharton
Hayley
H
Yardley
Vanessa
V
Moyna
Guillermo
G
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001372:Aza Compounds / Q000737:chemistry; D044946:Biflavonoids / Q000138:chemical synthesis* / Q000494:pharmacology*; D001643:Bridged Bicyclo Compounds / Q000737:chemistry; D002392:Catechin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D007893:Leishmania donovani / Q000187:drug effects*; D014349:Trypanosoma cruzi / Q000187:drug effects*
D000981:Antiprotozoal Agents; D001372:Aza Compounds; D044946:Biflavonoids; D001643:Bridged Bicyclo Compounds; C508389:benzotropolone; D002392:Catechin