Synthesis and Screening of New Antimalarial Drugs
Abstract
Eight new compounds were evaluated for radical curative properties in the rhesus P. cynomolgi model. Eight additional compounds are currently under-going evaluation. 2. WR238605 was evaluated in the three day casual prophylactic test and found to be protective with a calculated CD50 of 0.125 mg/kg/day (molar primaquine index of 10.5). An extensive protocol was also completed to evaluate a single dose regimen of WR238605 in the causal prophylactic model. This drug was protective at 2.84 mg/kg when given 2 days prior to sporozoite challenge and protective at 5.68 mg/kg when given 3 days prior to sporozoite challenge. These data correlate well with the known pharmacokinetics of the drug. 3. The blood schizonticidal properties of chloroquine (active at 3 mg/kg/day x 7 days) were validated in trophozoite-induced infections and WR238605 was found to be curative at doses at low as 1.0 mg/kg/day x 7 days. Keywords: RA 1; Antimalarial drugs; Drugs; Malaria; Plasmodium; India.
Document Details
- Document Type
- Technical Report
- Publication Date
- Oct 30, 1987
- Accession Number
- ADA206103
Entities
People
- M. M. Dhar
Organizations
- Central Drug Research Institute