期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 1, 期 9, 页码 460-465出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml100083c
关键词
Malaria; diarylurea
资金
- National Institute of Allergy and Infectious Disease at NIH [AI075517]
- American Lebanese Syrian Associated Charities (ALSAC)
- St. Jude Children's Research Hospital
- NATIONAL INSTITUTE OF ALLERGY AND INFECTIOUS DISEASES [U01AI075517] Funding Source: NIH RePORTER
A library of diarylurea insulin-like growth factor 1 receptor inhibitors was screened for activity against chloroquine-sensitive (3D7) and chloroquine-resistant (K1) strains of Plasmodium falciparum. The 4-aminoquinaldine-derived diarylureas displayed promising antimalarial potency. Further exploration of the B ring of 4-aminoquinaldinyl ureas allowed identification of several quinaldin-4-yl ureas 4{13, 39} and 4{13, 58) sufficiently potent against both 3D7 and K1 strains to qualify as bone fide leads.
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