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Synthesis of three classes of rhodacyanine dyes and evaluation of their in vitro and in vivo antimalarial activity |
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| Authors: | Pudhom Khanitha Kasai Kazuki Terauchi Hiroki Inoue Hiroshi Kaiser Marcel Brun Reto Ihara Masataka Takasu Kiyosei |
| Affiliation: | aDepartment of Organic Chemistry, Graduate School of Pharmaceutical Sciences, Tohoku University, Aobayama, Sendai 980-8578, Japan bJapan Science and Technology Agency (JST), 5-3 Yonbanchou, Chiyoda-ku, Tokyo 102-8666, Japan cDepartment of Chemistry, Faculty of Science, Chulalongkorn University, Phayathai Road, Patumwan, Bangkok 10330, Thailand dSwiss Tropical Institute, Socinstrasse 57, CH-4002 Basel, Switzerland eHoshi University, 2-4-41 Ebara, Shinagawa-ku, Tokyo 142-8501, Japan |
| Abstract: | Selected members of three classes of rhodacyanine dyes, [0, 0]-, [1, 0]-, and [0, 0, 0]-rhodacyanines, were synthesized and their in vitro antimalarial activities against Plasmodium falciparum K1 (chloroquine-resistant strain) as well as their in vivo activities against P. berghei in mice were determined. The novel [0, 0, 0]-rhodacynines, 3e and 3h, possessing a benzothiazole moiety, were shown to have highly promising antimalarial activities in vivo. Moreover, the [0, 0, 0]-rhodacyanines were found to be orally bioavailable. |
| Keywords: | Malaria Rhodacyanines DLC hypothesis Drug resistance |
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