title: Synthesis and in vitro antiprotozoal activities of water-soluble, inexpensive 3,7-bis(dialkylamino)phenoxazin-5-ium derivatives.
abstract: 3,7-Bis(dialkylamino)phenoxazinium salts were synthesized and evaluated for in vitro activities against Plasmodium falciparum, Trypanosoma cruzi, T. brucei rhodesiense, and Leishmania donovani. Notably, the compounds showed potent antiprotozoal activities, especially against P. falciparum and T. cruzi. The compounds with alkyl side chains less than three carbons in length possessed good activities with high selective indices.
authors.affiliation: Institute of Medicinal Chemistry, Hoshi University, 2-4-41 Ebara, Shinagawa-ku, Tokyo 142-8501, Japan.
authors.forename: Jian-Feng
authors.initials: JF
authors.lastname: Ge
authors.forename: Chika
authors.initials: C
authors.lastname: Arai
authors.forename: Marcel
authors.initials: M
authors.lastname: Kaiser
authors.forename: Sergio
authors.initials: S
authors.lastname: Wittlin
authors.forename: Reto
authors.initials: R
authors.lastname: Brun
authors.forename: Masataka
authors.initials: M
authors.lastname: Ihara
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002738:Chloroquine / Q000494:pharmacology; D004351:Drug Resistance; D007893:Leishmania donovani / Q000187:drug effects; D010078:Oxazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects; D011739:Pyrimethamine / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D016833:Trypanosoma brucei rhodesiense / Q000187:drug effects; D014349:Trypanosoma cruzi / Q000187:drug effects
chemical_list: D000962:Antimalarials; D000981:Antiprotozoal Agents; D010078:Oxazines; D014344:Trypanocidal Agents; D002738:Chloroquine; D011739:Pyrimethamine