title: Synthesis and in vitro protozoocidal evaluation of novel diazabicyclic tropolone derivatives.
abstract: The synthesis and in vitro antiparasitic activity of twenty-seven novel diazabicycles based on tropolone ethers is presented. The compounds can be readily prepared by means of a high-yielding hetero Diels-Alder reaction using simple and readily available starting materials. Several of the new diazabicycles have in vitro activities against Trypanosoma cruzi, Leishmania donovani, Trypanosoma brucei rhodesiense, and chloroquine-resistant Plasmodium falciparum that are comparable or superior to those of currently employed protozoocidal agents.
authors.affiliation: Department of Chemistry & Biochemistry, University of Sciences in Philadelphia, Philadelphia, PA 19104-4495, USA.
authors.forename: Alexander
authors.initials: A
authors.lastname: Khrizman
authors.forename: Rachel D
authors.initials: RD
authors.lastname: Slack
authors.forename: Richard C
authors.initials: RC
authors.lastname: Remsing
authors.forename: Susan
authors.initials: S
authors.lastname: Little
authors.forename: Vanessa
authors.initials: V
authors.lastname: Yardley
authors.forename: Guillermo
authors.initials: G
authors.lastname: Moyna
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000009:adverse effects / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D053961:Azabicyclo Compounds / Q000009:adverse effects / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D056890:Eukaryota / Q000187:drug effects*; D006801:Humans; D007624:KB Cells; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship; D014334:Tropolone / Q000031:analogs & derivatives*
chemical_list: D000981:Antiprotozoal Agents; D053961:Azabicyclo Compounds; D014334:Tropolone