title: Design, synthesis, and evaluation of potential prodrugs of DFMO for reductive activation.
abstract: A series of potential DFMO prodrugs was designed through the incorporation of 4-nitrobenzyl ester or carbamate groups for potential activation by trypanosomal nitroreductase. It was found that only modification of N(ε)-amino group of DFMO by 4-nitro-2-fluorobenzyloxycarbonyl resulted in significant trypanocidal activity and could serve as a lead for further investigation.
authors.affiliation: Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, NJ 08854, USA.
authors.forename: Yanhui
authors.initials: Y
authors.lastname: Yang
authors.forename: Andrew
authors.initials: A
authors.lastname: Voak
authors.forename: Shane R
authors.initials: SR
authors.lastname: Wilkinson
authors.forename: Longqin
authors.initials: L
authors.lastname: Hu
mesh_terms: D001665:Binding Sites; D015195:Drug Design; D008954:Models, Biological; D009601:Nitroreductases / Q000378:metabolism; D010084:Oxidation-Reduction; D011355:Prodrugs / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D014345:Trypanosoma / Q000187:drug effects* / Q000201:enzymology
chemical_list: D011355:Prodrugs; D014344:Trypanocidal Agents; D009601:Nitroreductases