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Zheng, Yang; Matheeussen, An; Maes, Louis; Caljon, Guy; Sterk, Geert Jan; Leurs, Rob
Molecules (Basel, Switzerland), 06/2023, Letnik: 28, Številka: 13Journal Article
Malaria continues to pose a significant health threat, causing thousands of deaths each year. The limited availability of vaccines and medications, combined with the emergence of drug resistance, further complicates the fight against this disease. In this study, we aimed to enhance the antimalarial potency of the previously reported hit compound BIPPO (pIC 5.9). Through systematic modification of pyrazolopyrimidinone analogs, we discovered the promising analog (NPD-3547), which exhibited approximately one log unit higher in vitro potency (pIC 6.8) against . Furthermore, we identified several other BIPPO analogs ( , , and ) with potent antimalarial activity (pIC > 6.0) and favorable metabolic stability in mouse liver microsomes. These compounds can serve as new tools for further optimization towards the development of potential candidates for antimalarial studies.
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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Vir: Osebne bibliografije
in: SICRIS
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