Advisor Information
James Hagen
Location
Dr. C.C. and Mabel L. Criss Library
Presentation Type
Poster
Start Date
3-3-2017 2:15 PM
End Date
3-3-2017 3:30 PM
Abstract
Demand for novel chemotherapeutic agents that treat Human African Trypanosomaiasis (HAT) persists. A series of compounds sharing a 3,4’diphephyl ether skeleton were prepared for a structure activity relationship (SAR) study evaluating antitrypansomal drug candidates. Trypanocidal assays performed in vitro by the Swiss Tropical and Public Health Institute identified a lead with an IC50 of 1.35 μg/mL analogous to a compound previously made in our laboratory. A slight improvement in activity (10%) was observed when changing the molecular substitution pattern from 4,4’ to 3,3’; however, the result is equivocal. Furthermore, in vitro test results demonstrated the weakness of amides as side chain functional groups, emphasizing the role of cationic moieties.
Synthesis of Small Molecule Anti-Trypanosomal Drugs
Dr. C.C. and Mabel L. Criss Library
Demand for novel chemotherapeutic agents that treat Human African Trypanosomaiasis (HAT) persists. A series of compounds sharing a 3,4’diphephyl ether skeleton were prepared for a structure activity relationship (SAR) study evaluating antitrypansomal drug candidates. Trypanocidal assays performed in vitro by the Swiss Tropical and Public Health Institute identified a lead with an IC50 of 1.35 μg/mL analogous to a compound previously made in our laboratory. A slight improvement in activity (10%) was observed when changing the molecular substitution pattern from 4,4’ to 3,3’; however, the result is equivocal. Furthermore, in vitro test results demonstrated the weakness of amides as side chain functional groups, emphasizing the role of cationic moieties.