In vitro efficacy of 7-benzylamino-1-isoquinolinamines against Plasmodium falciparum related to the efficacy of chalcones

CE Gutteridge, MM Hoffman, AK Bhattacharjee…

文献索引：Gutteridge, Clare E.; Hoffman, Marshall M.; Bhattacharjee, Apurba K.; Milhous, Wilbur K.; Gerena, Lucia Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 2 p. 786 - 789

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被引用次数: 9

摘要

A series of 1, 7-diaminoisoquinolinamines, that are expected to mediate antimalarial activity by the same mechanism employed by the chalcones, were produced. Six 7-benzylamino-1- isoquinolinamines were found to be submicromolar inhibitors in vitro of drug-resistant Plasmodium falciparum, with the best possessing activity comparable to chloroquine. Despite being developed from a lead that is a DHFR inhibitor, these compounds do not ...