Synthesis and Biological Evaluation of Some Potential Antimalarials. Synthese und biologische Bewertung einiger potentieller Wirkstoffe gegen Malaria
✍ Scribed by Chang Swei Tsai; Ai Yu Shen
- Publisher
- John Wiley and Sons
- Year
- 1994
- Tongue
- English
- Weight
- 213 KB
- Volume
- 327
- Category
- Article
- ISSN
- 0365-6233
No coin nor oath required. For personal study only.
✦ Synopsis
Malaria chemotherapy has been well re~iewedl-~). Malarial parasites gaining resistance is the major problem in the treatment of the disease. Some strains are resistant not only to chloroquine but also to amodiaquine. Few new drugs are available or foreseen for the near f u t ~r e ~-~) .
The principal metabolite of cinchona alkaloids appears to be oxidized at C-2. This may result in a loss of activity. Pinder and Burger suggested that a mfluoromethyl group will prevent this oxidation6). So 2-tribromomethyl-6-methoxy-4-(4-hydroxy-3-pyrrolidinomethylanilino)quinoline (1) was synthesized as a potential biocide (Scheme 1).