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Odawara, Japan

Ge J.-F.,Hoshi University | Ge J.-F.,Soochow University of China | Arai C.,Hoshi University | Yang M.,Hoshi University | And 12 more authors.
ACS Medicinal Chemistry Letters | Year: 2010

Malaria is a serious infectious disease caused by protozoan parasites in tropical and subtropical regions. Even inhabitants of temperate zones are exposed to the danger of malaria infection because of travel and global warming. Novel, effective, safe, and inexpensive drugs are required to treat malaria and contribute to the global goal of eradication. A search for new antimalarial agents has been performed by the synthesis of new benzo[a]phenoxazines, followed by biological evaluations. The derivative SSJ-183 (5), having a 4-aminopyridine group, showed an IC50 value against Plasmodium falciparum of 7.6 nM and a selectivity index of >7300. Cure was achieved by three oral doses of 5 at 100 mg/kg to mice infected with the Plasmodium berghei ANKA strain. The safety of 5 was supported by acute toxicity testing in mice with single doses up to 2000 mg/kg po, chromosome aberration test, in vitro as well as in vivo micronucleus tests, and phototoxicity studies in mice. Thus, 5 is a promising candidate as a new antimalarial agent. © 2010 American Chemical Society. Source

Mizukawa Y.,Hoshi University | Mizukawa Y.,Synstar Japan Co. | Ge J.-F.,Hoshi University | Ge J.-F.,Soochow University of China | And 12 more authors.
Bioorganic and Medicinal Chemistry | Year: 2014

A productive synthesis of benzo[a]phenoxazine derivative SSJ-183 (1), a promising lead for antimalarial agents, was developed using a one pot procedure. Furthermore, N-deethylated metabolite 3 and bis-N,N-deethylated metabolite 4 were synthesized by the application of the method. The metabolites 3 and 4 showed comparable and ∼2-fold increased activities against drug-sensitive and drug-resistant Plasmodium falciparum parasites. © 2014 Elsevier Ltd. All rights reserved. Source

Yang M.,Hoshi University | Arai C.,Hoshi University | Bakar Md. A.,Hoshi University | Lu J.,Hoshi University | And 12 more authors.
Journal of Medicinal Chemistry | Year: 2010

Anti-Leishmania in vitro and in vivo activities of various rhodacyanine derivatives have been examined. Among them, the fluorinatied variant SJL-01 (8) showed IC50 of 0.011 μMagainst Leishmania donovani strain MHOM/ET/67/L82 (selective index of > 15000) and 95-97% inhibition against L. donovani strainMHOM/ET/67/HUin female BALB/c mice by 1.3-12.5 mg/kg x 5 iv administrations. Negative results on chromosomal aberration test and in vitro micronucleus test suggest that compound 8 is a hopeful candidate for visceral leishmaniasis (VL). ©2009 American Chemical Society. Source

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