Category: alcohols-buliding-blocksIn 2021 ,《Discovery of fast-acting dual-stage antimalarial agents by profiling pyridylvinylquinoline chemical space via copper catalyzed azide-alkyne cycloadditions》 appeared in European Journal of Medicinal Chemistry. The author of the article were Huang, Guang; Solano, Claribel Murillo; Melendez, Joel; Yu-Alfonzo, Sabrina; Boonhok, Rachasak; Min, Hui; Miao, Jun; Chakrabarti, Debopam; Yuan, Yu. The article conveys some information:
The identity of fast-acting, multistage antimalarial agents, a series of pyridylvinylquinoline-triazole analogs I (R = pyrrolidin-1-yl, diethylamino, 4-methylpiperazin-1-yl, 1,3-dioxo-2,3-dihydro-1H-isoindol-2-yl, etc.) and II (R1 = piperidin-1-yl, 2-(piperazin-1-yl)ethan-1-ol, 1H-pyrazol-1-yl, (5Z)-2,4-dioxo-5-(phenylmethylidene)-1,3-thiazolidin-3-yl, etc.; n = 1, 2) have been synthesized via CuAAC. Most of the compounds display significant inhibitory effect on the drug-resistant malarial Dd2 strain at low submicromolar concentrations Among the tested analogs, compound II (R1 = piperidin-1-yl; n = 2) is the most potent mol. with an EC50 value of 0.04 ± 0.01 mM. This study indicates that compound II (R1 = piperidin-1-yl; n = 2) is a fast-acting antimalarial compound and it demonstrates stage specific action at the trophozoite phase in the P. falciparum asexual life cycle. In addition, compound II (R1 = piperidin-1-yl; n = 2) is active against both early and late stage P. falciparum gametocytes. From a mechanistic perspective, compound II (R1 = piperidin-1-yl; n = 2) shows good activity as an inhibitor of β-hematin formation. Collectively, the findings suggest that fast-acting agent II (R1 = piperidin-1-yl; n = 2) targets dual life stages of the malarial parasites and warrant further investigation of pyridylvinylquinoline hybrids as new antimalarials. In the experiment, the researchers used many compounds, for example, 4-Aminobutan-1-ol(cas: 13325-10-5Category: alcohols-buliding-blocks)
4-Aminobutan-1-ol(cas: 13325-10-5) is used in the synthesis of NSAIDs with anti-inflammatory properties. Also used in the synthesis of polyamine transport ligands with specificity against human cancers allowing easy access to specific cancer cells.Category: alcohols-buliding-blocks
Referemce:
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Alcohols – Chemistry LibreTexts