Nicotinic acid hydrazide was incorporated into new 4,5-dihydro-5-hydroxy-3,5-diphenylpyrazol-1-yl derivatives. Compounds 6a-h were synthesized, and their antihyperlipidemic activity was evaluated in high cholesterol diet-fed rat model. Compounds 6e, 6f were found to decrease the levels of serum total cholesterol by 14-19% compared to control group. Total triglycerides were also reduced by 24-28% and LDL cholesterol by 16%. As expected from parent niacin, compounds 6e and 6f caused an elevation of HDL cholesterol by 33-41%. Docking study supported the ability of designed compounds to block NPC1L1 active site in a manner similar to that observed with ezetimibe.

中文翻译：

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新型烟酸基 3,5-二苯基吡唑：设计、合成和抗高血脂活性，具有潜在的 NPC1L1 抑制活性。


烟酸酰肼被引入新的4,5-二氢-5-羟基-3,5-二苯基吡唑-1-基衍生物中。合成了化合物6a-h，并在高胆固醇饮食喂养的大鼠模型中评价了它们的抗高血脂活性。发现与对照组相比，化合物6e、6f使血清总胆固醇水平降低14-19%。总甘油三酯也降低了 24-28%，低密度脂蛋白胆固醇降低了 16%。正如母体烟酸所预期的那样，化合物 6e 和 6f 导致 HDL 胆固醇升高 33-41%。对接研究支持设计的化合物能够以与依折麦布观察到的类似方式阻断 NPC1L1 活性位点。