title: Synthesis and antimalarial activity of thioetherhydroxyethylsulfonamides, potential aspartyl protease inhibitors, Part 3.
abstract: A series of novel thioetherhydroxyethylsulfonamide derivatives has been synthesized from the coupling of intermediates 3-amino-4-phenyl-1-thioetherazine-butan-2-oles 6,7 with arenesulfonyl chlorides in good yields. Characterizations of products were achieved by NMR techniques and specifically for compound 8e by X-ray crystallography. Preliminary results of antimalarial activity in vitro against the Plasmodium falciparum W2 clone (chloroquine resistant and mefloquine sensitive) showed moderate activity for hydroxyethylsulfonamide 8f. In addition, none of the compounds tested showed cytotoxicity at high concentration tested against HepG2 and BGM cell lines.
authors: Universidade Federal Fluminense, Instituto de Química, Departamento de Química Orgânica, Centro, Niterói 24020-141, RJ, Brazil.
authors: Walcimar T
authors: WT
authors: Vellasco Junior
authors: Guilherme P
authors: GP
authors: Guedes
authors: Thatyana R A
authors: TR
authors: Vasconcelos
authors: Maria G F
authors: MG
authors: Vaz
authors: Marcus V N
authors: MV
authors: de Souza
authors: Antoniana U
authors: AU
authors: Krettli
authors: Luisa G
authors: LG
authors: Krettli
authors: Anna Caroline C
authors: AC
authors: Aguiar
authors: Claudia R B
authors: CR
authors: Gomes
authors: Wilson
authors: W
authors: Cunico
mesh_terms: D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D057055:Aspartic Acid Proteases / Q000037:antagonists & inhibitors*; D060326:Chemistry Techniques, Synthetic; D056945:Hep G2 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D008958:Models, Molecular; D008968:Molecular Conformation; D010963:Plasmodium falciparum / Q000187:drug effects; D011480:Protease Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D000962:Antimalarials; D011480:Protease Inhibitors; D013449:Sulfonamides; D057055:Aspartic Acid Proteases