抗氯喹变构体和连接子变体：抗疟原虫活性。
Reversal agent and linker variants of reversed chloroquines: activities against Plasmodium falciparum.
机构信息
Department of Chemistry, Portland State University, P.O. Box 751, Portland, Oregon 97207-0751, USA.
出版信息
J Med Chem. 2010 Jan 28;53(2):916-9. doi: 10.1021/jm900972u.
Abstract
We have shown that "reversed chloroquine molecules" constructed from chloroquine-like and resistance "reversal-agent"-like cores can be powerful drugs against malaria ( J. Med. Chem. 2006 , 49 , 5623 - 5625 ). Several reversed chloroquines are now presented that probe parameters governing the activities against chloroquine-resistant and chloroquine-sensitive malaria strains. The design is tolerant to linker and reversal agent changes, but a piperazinyl group adjacent to the quinoline, at least for the group of compounds studied here, may be detrimental.
摘要
我们已经证明，由氯喹类似物和耐药“逆转剂”类似物核心构建的“反向氯喹分子”可以成为对抗疟疾的有力药物（J. Med. Chem. 2006, 49, 5623-5625）。现在提出了几种反向氯喹，以研究控制抗氯喹和敏感疟疾菌株活性的参数。该设计对连接子和逆转剂的变化具有耐受性，但至少对于我们在这里研究的化合物组，毗邻喹啉的哌嗪基可能是有害的。
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