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Synthesis and Biological Evaluation of Some Potential Antimalarials. Synthese und biologische Bewertung einiger potentieller Wirkstoffe gegen Malaria
Author(s) -
Tsai Chang Swei,
Shen Ai Yu
Publication year - 1994
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19943271015
Subject(s) - amodiaquine , malaria , chemistry , metabolite , quinoline , chloroquine , cinchona alkaloids , nitrofuran , stereochemistry , pharmacology , biochemistry , biology , organic chemistry , catalysis , immunology , enantioselective synthesis , genetics
Malaria chemotherapy has been well reviewed. 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 future. 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 trifluoromethyl group will prevent this oxidation. So 2‐tribromomethyl‐6‐methoxy‐4‐(4‐hydroxy‐3‐pyrrolidinomethylanilino)quinoline ( I ) was synthesized as a potential biocide (Scheme 1).