The Synthesis of Potential Parasitic Drugs
Abstract
During the period from 1 April 1988 to 31 March 1989, we submitted to WRAIR 8 target compounds (Table I) and 15 intermediates (Table II). A number of additional syntheses are in progress (Table III). In earlier work, we prepared a series of primaquines with a methyl group at position 4 and a phenylalkoxy group at position 5. These compounds combined low toxicity with a unique dual efficacy against the blood and tissue forms of the malarial parasite. (Tables VI and VII) . In the past year, we have attempted to enhance this series by attaching various substituents to the phenyl portion of the 5-phenylalkoxy group. Screening data for the new compounds are still too sparse for SAR conclusions (Tables IV & V). While awaiting additional data, we have started work on another groups of primaquines. These derivatives will have an alkoxy, phenoxy, or benzyloxy group at position 5, a methyl group at positions 3 or 4 and a methoxy or methyl group at position 2. Keywords: Antiparasitic drugs, Antimalarials, Primaquine, SAR, 8-Aminoquinolines, Blood schizontocides, Tissue schizontocides, Syntheses, RAI.
Document Details
- Document Type
- Technical Report
- Publication Date
- May 01, 1989
- Accession Number
- ADB135200
Entities
People
- Edward A. Nodiff
- Keiichi Tanabe
- Sankar Chattopadhyay