1236000-85-3Relevant academic research and scientific papers
Synthesis, characterization, molecular structure, and computational studies on 4(1H)-pyran-4-one and its derivatives
Ajani, Olayinka O.,Audu, Oluwatosin Yemisi,Jooste, Jessica,Malan, Frederick P.,October, Natasha
, (2021)
4(1H)-Pyridone-based compounds have shown promise as potent bioactive inhibitors against a broad range of diseases, particularly malaria. Our interest in 4(1H)-pyridones initiated the design and synthesis of a series of 4(1H)-pyridone derivatives, with th
In silico design, chemical synthesis and biological screening of novel 4-(1H)-pyridone-based antimalarial agents
Audu, Oluwatosin,Stander, Andre,Ajani, Olayinka,Egieyeh, Samuel,October, Natasha
, p. 674 - 687 (2022/02/02)
Identifying novel lead compounds in drug discovery has been challenging because of the rapid rise of drug resistance to the existing chemotherapeutics and a lack of understanding of complex metabolic pathways in the parasite. Integrating computational and experimental approaches has shown to be of great worth in identifying and developing novel promising pharmacophore hybrids. In this present research, a series of new 4-(1H)-pyridone-derived antimalarial agents were designed based on recent reports and our preliminary findings through in silico studies. Two of the 4-(1H)-Pyridone derivatives showed potential to bind to the Q0 site of the cytochrome bc1 complex and disrupt the mitochondrial electron transport chain. These compounds, along with previously synthesized compounds, exhibited significant inhibitory activities against the malaria parasite. Presently, seven compounds were successfully synthesized, characterized and these novel compounds have shown promise as antimalarial agents.
4 ( 1H) -PYRIDINONE DERIVATIVES AND THEIR USE AS ANTIMALARIA AGENTS
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Page/Page column 52, (2010/08/08)
4-pyridone (4-pyridinone) derivatives of Formula (I) and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of certain parasitic infections such as malaria, are provided.
