Chemotherapy of malaria

Abstract

OF the hundreds of 4-aminoquinolines tried against malaria, two classes of compounds have been found to show good therapeutic action: (1) those having an aliphatic side chain terminating in an alkylamino group, such as chloroquin or oxychloroquin, and (2) those having a benzene ring bearing further basic substituents, such as " camoquin " (I). The compounds of second group are easier to synthesise and also manufacture, but the possibilities in this direction have not been fully explored. The attempts to synthesise quinoline derivatives with a guanidine or biguanide side chain at the position 4 having proved a failure as shown in the previous part, as the next best, the synthesis of 4-phenylaminoquinoline derivatives with a guanidine radical substituted in the benzene ring (II) was taken up. This paper records the attempts made to work out a general method of synthesis of compounds of type (II) which could be used to synthesise a variety of quinolines.