Enhanced Pneumocystis carinii activity of new primaquine analogues

New analogues of the venerable antimalarial drug primaquine have been synthesized and bioassayed in vivo against Pneumocystis carinii, a life-threatening infection common among immunosuppressed patients. Two of these new compounds are significantly more active than primaquine itself, and provide new...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2000-10, Vol.10 (19), p.2205-2208
Main Authors: Goodwin, Thomas E, Boylan, Carole J, Current, William L, Byrd, John C, Edwards, Clint B, Fuller, Danny A, Green, Jennifer L, Larocca, Christine D, Raney, Kevin D, Ross, Ashley S, Tucker, W.Andrew
Format: Article
Language:English
Subjects:
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antifungal agents
Antifungal Agents - chemical synthesis
Antifungal Agents - chemistry
Antifungal Agents - pharmacology
Antifungal Agents - therapeutic use
Biological and medical sciences
Dose-Response Relationship, Drug
Drug Design
Female
Humans
Medical sciences
Molecular Structure
Pharmacology. Drug treatments
Pneumocystis - drug effects
Pneumocystis Infections - drug therapy
Primaquine - analogs & derivatives
Primaquine - chemical synthesis
Primaquine - chemistry
Primaquine - pharmacology
Primaquine - therapeutic use
Rats
Structure-Activity Relationship
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Summary:New analogues of the venerable antimalarial drug primaquine have been synthesized and bioassayed in vivo against Pneumocystis carinii, a life-threatening infection common among immunosuppressed patients. Two of these new compounds are significantly more active than primaquine itself, and provide new information for future drug design and development in this area.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00436-4