Isolation and antimalarial activity of peroxydisulfate oxidation products of primaquine

• Published in: Bioorganic & medicinal chemistry letters 2002-12, Vol.12 (24), p.3587-3589
• Main Authors: Dua, Virendra K, Sinha, Sukesh N, Biswas, Sukla, Valecha, N, Puri, S.K, Sharma, V.P
• Format: Article
• Language: English
• Subjects: Animals; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antimalarials - chemistry; Antimalarials - isolation & purification; Antimalarials - pharmacology; Antiparasitic agents; Biological and medical sciences; Culicidae - microbiology; Germ Cells - drug effects; Malaria - drug therapy; Medical sciences; Mice; Oocysts - drug effects; Oxidation-Reduction; Pharmacology. Drug treatments; Plasmodium yoelii - drug effects; Primaquine - chemistry; Sulfates - chemistry
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/S0960-894X(02)00802-8

Five compounds formed by peroxydisulfate oxidation of primaquine were isolated using chromatographic methods and evaluated for antimalarial activity in vitro. One compound 6-methoxy-5,8 bis(4′-amino-1′-methylbutylamino)quinoline [ P 1 ] was found to have good gametocytocidal activity against Plasmodium yoelli infected mice at 10 mg kg −1 dose in vivo. Five compounds formed by peroxydisulfate oxidation of primaquine were isolated using chromatographic methods and evaluated for antimalarial activity in vitro. One compound 6-methoxy-5,8 di-(4′-amino-1′-methylbutyl-amino)-quinoline [ P 1 ] was found to have good gametocytocidal activity against Plasmodium yoelli infected mice at 10 mg kg −1 dose in vivo.