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Inhibitory effects of 9‐anilinoacridines on Plasmodium falciparum gametocytes
Author(s) -
ChavalitshewinkoonPetmitr P.,
Pongvilairat G.,
Ralph R. K.,
Denny W. A.,
Wilairat P.
Publication year - 2001
Publication title -
tropical medicine and international health
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.056
H-Index - 114
eISSN - 1365-3156
pISSN - 1360-2276
DOI - 10.1046/j.1365-3156.2001.00656.x
Subject(s) - gametocyte , plasmodium falciparum , parasite hosting , biology , in vitro , apicomplexa , malaria , drug , virology , pharmacology , immunology , biochemistry , world wide web , computer science
Summary Two gametocyte‐producing isolates of Plasmodium falciparum , KT1 and KT3, were cultivated in vitro . On day 11 of cultivation, pure gametocytes containing stage II, III and IV were used to test the gametocytocidal activity of 9‐anilinoacridines that had previously demonstrated their activity against the asexual stage of the parasite. After drug exposure for 48 h, gametocytes were maintained without drugs for another 2 days before thin films were prepared for parasite counting. Gametocytocidal activities of 13 analogs of 9‐anilinoacridine were observed with 50% inhibitory concentrations in the range of 0.6 μ m to > 100 μ m . The most active compound was 1′‐CH 2 NMe 2 ‐9‐anilinoacridine. Anilinoacridine derivatives with 3,6‐diamino substitution had reduced gametocytocidal activity in contrast to their enhancing effect against the asexual forms. Morphological abnormalities of gametocytes were observed following drug exposure.