Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:18

Article

Vale, Nuno¹  Collins, Margaret S.³  Gut, Jiri⁴  Ferraz, Ricardo^1,2  Rosenthal, Philip J.⁴  Cushionc, Melanie T.³  Gomes, Paula¹ 

[1] Univ Porto, Ctr Invest Quim, Dept Quim, Fac Ciencias, P-4169 Oporto, Portugal

[2] Inst Politecn Porto, Escola Super Tecnol Saude Porto, P-4000 Oporto, Portugal

[3] Univ Cincinnati, Dept Internal Med, Div Infect Dis, Cincinnati, OH 45267 USA

[4] Univ Calif San Francisco, San Francisco Gen Hosp, Dept Med, San Francisco, CA 94143 USA

关键词: AIDS;    antimalarial;    antiplasmodial;    HIV;    infection;    malaria;    plasmodium falciparum;    pneumocystis carinii;    primaquine;   

DOI  :  10.1016/j.bmcl.2007.11.105

来源: Elsevier

【 摘 要 】

A series of primaquine-derived imidazolidin-4-ones were screened for their in vitro activity against Pneumocystis carinii and Plasmodium falciparum W2 strain. Most compounds were active against P. carinii above 10 mu g/mL and displayed slight to marked activity. The imidazolidin-4-ones most active against P. carinii were also those most active antiplasmodial agents, in the mu M range. One of the tested imidazolidin-4-ones was slightly more active than the parent primaquine and may represent a lead compound for the development of novel anti-P. carinii 8-aminoquinolines with increased stability and resistance to metabolic inactivation. (c) 2007 Elsevier Ltd. All rights reserved.

【 授权许可】

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