H

17 axisonitrile-3

18 diisocyanoadociane

17 axisonitrile-3

18 diisocyanoadociane is an anhydronium base), and this may be important for its biological activity. The 7-nitro-, 7,9-dinitro-, and 7-N-acetyl- derivatives were of similar antiplasmodial activity to the parent while 9-nitrocryptolepine was 10-fold less potent. Improved antiplasmodial activities were seen with the 2-bromo- and 7-bromo- analogues, and this prompted the synthesis of 2,7-dibromocryptolepine, which was ninefold more potent than cryptolepine. Interestingly, although 11-chlorocryptolepine was twice as potent as cryptolepine, a number of dihalogenated derivatives that were 11-chloro-substituted, including 2-bromo, 11-chlorocryptolepine, were found to have weak antiplasmodial activities.

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