1391426-22-4Relevant articles and documents
Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed to Have Multiple Interactions with Heme
Sakata, Yosuke,Yabunaka, Kosuke,Kobayashi, Yuko,Omiya, Hirohisa,Umezawa, Naoki,Kim, Hye-Sook,Wataya, Yusuke,Tomita, Yoshimi,Hisamatsu, Yosuke,Kato, Nobuki,Yagi, Hirokazu,Satoh, Tadashi,Kato, Koichi,Ishikawa, Haruto,Higuchi, Tsunehiko
, p. 980 - 985 (2018)
Based on the idea that compounds designed to exhibit high affinity for heme would block hemozoin formation, a critical heme-detoxification process for malarial parasites, we synthesized a series of compounds with two π-conjugated moieties at terminal amino groups of triamine. These compounds exhibited moderate to high antimalarial activities in vitro toward both chloroquine-sensitive and chloroquine-resistant Plasmodium falciparum. In a P. berghei-infected mouse model, 3a and 12a showed potent antimalarial activities compared to artesunate, as well as a prolonged duration of antimalarial effect. We found a good correlation between protective activity against hemin degradation and antimalarial activity. Compounds 8b and 3a strongly inhibited hemozoin formation catalyzed by heme detoxification protein.
NOVEL BISAMINOQUINOLINE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS PREPARED THEREFROM AND THEIR USE
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Page/Page column 33; 34, (2012/11/13)
The present invention relates to novel bisaminoquinoline compounds, pharmaceutical compositions comprising these novel compounds and methods for inhibiting autophagy in biological systems. Methods of treating cancer in patients in need using compounds and/or compositions according to the present invention alone or in combination with at least one additional anticancer agent represent additional aspects of the invention. Methods of treating disease states and/or conditions in which inhibition of autophagy plays a favorable treatment role including rheumatoid arthritis, malaria, antiphospholipid antibody syndrome, lupus, chronic urticaria and Sjogren's disease, with compounds according to the present invention represent additional aspects of the invention.