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Aldose reductase (AR) acts as a multi-disease target for the design and development of therapeutic agents for the management of diabetic complications as well as non-diabetic diseases. In the search for potent AR inhibitors, the microwave-assisted synthesis of twenty new compounds with a 1,3-diaryl-5-(4-fluorophenyl)-2-pyrazoline moiety as a common fragment in their structure (1–20) was carried out efficiently. Compounds 1–20 were subjected to in vitro studies, which were conducted to assess their AR inhibitory effects and cytotoxicity towards L929 mouse fibroblast (normal) cells. Among these compounds, 1-(3-bromophenyl)-3-(4-piperidinophenyl)-5-(4-fluorophenyl)-2-pyrazoline (20) was identified as the most promising AR inhibitor with an IC₅₀ value of 0.160 ± 0.005 μM exerting competitive inhibition with a K_i value of 0.019 ± 0.001 μM as compared to epalrestat (IC₅₀ = 0.279 ± 0.001 μM; K_i = 0.801 ± 0.023 …