Journal
ACS INFECTIOUS DISEASES
Volume 4, Issue 4, Pages 577-591Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsinfecdis.7b00212
Keywords
drug repurposing; tropical diseases; malaria; target class repurposing
Categories
Funding
- National Institutes of Health [R01AI082577, R56AI099476, R01AI124046, R21AI127594]
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We recently reported the medicinal chemistry reoptimization of a known human tyrosine kinase inhibitor, lapatinib, against a variety of parasites responsible for numerous tropical diseases, including human African trypanosomiasis (Trypanosoma brucei), Chagas disease (T. cruzi), Leishmaniasis (Leishmania spp.), and malaria (Plasmodium falciparum). Herein, we report our continuing efforts to optimize this series against P. falciparum. Through the design of a library of compounds focused on reducing the lipophilicity and molecular weight, followed by an SAR exploration, we have identified NEU-1953 (40). This compound is a potent inhibitor of P. falciparum with an improved ADME profile over the previously reported compound, NEU-961 (3).
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