Synthesis of New Antimalarial Agents.
Abstract
The study presented in this report is concerned with the preparation of: (a) peroxides based on qinghaosu, (b) peptide derivatives of primaquine, and (c) thymidylate synthetase inhibitors as potentially new antimalarial agents. During the first year of this study, twelve (12) target compounds were prepared and submitted for antimalarial evaluation. The twelve compounds included eight (8) qinghaosu analogs, one (1) primaquine derivative and three (3) thymidylate synthetase inhibitors. Two of the qinghaosu analogs and all three of the thymidylate synthetase inhibitors were evaluated in the malaria in vitro drug screen. The qinghaosu analogs showed reasonable activity in this screen, whereas the thymidylate synthetase inhibitors were inactive. The primaquine peptide showed sufficient activity in the preliminary prophylactic screen to warrant its submission to the monkey P. cynomolgi screen.
Document Details
- Document Type
- Technical Report
- Publication Date
- May 01, 1984
- Accession Number
- ADB101584
Entities
People
- Frank I. Carroll
- John A. Kepler
Organizations
- RTI International