期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 3, 期 5, 页码 373-377出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml300008j
关键词
indoline; malaria; Tres Cantos Antimalarial set; divergent SAR; open-innovation
资金
- Medicines for Malaria Venture (MMV)
From the 13 533 chemical structures published by GlaxoSmithKline in 2010, we identified 47 quality starting points for lead optimization. One of the most promising hits was the TCMDC-139046, a molecule presenting an indoline core, which is well-known for its anxiolytic properties by interacting with serotonin antagonist receptors 5-HT2. The inhibition of this target will complicate the clinical development of these compounds as antimalarials. Herein, we present the antimalarial profile of this series and our efforts to avoid interaction with this receptor, while maintaining a good antiparasitic potency. By using a double-divergent structure-activity relationship analysis, we have obtained a novel lead compound harboring an indoline core.
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