Zlatanova-Tenisheva Hristina, Vladimirova Stanislava
Department of Pharmacology and Clinical Pharmacology, Medical University of Plovdiv, 4002 Plovdiv, Bulgaria.
Department of Organic Synthesis, University of Chemical Technology and Metallurgy, 1756 Sofia, Bulgaria.
Molecules. 2025 Mar 26;30(7):1472. doi: 10.3390/molecules30071472.
Hydrazones, characterized by their C=N-NH functional group, are promising candidates in medicinal chemistry due to their ability to interact with biological targets. This study evaluated the anti-inflammatory and analgesic properties of -pyrrolylcarbohydrazide () and four pyrrole hydrazone derivatives () in male Wistar rats (6 weeks old). Anti-inflammatory activity was assessed using a carrageenan-induced paw edema model, while formalin, tail flick, and paw withdrawal tests evaluated analgesia. Compound exhibited dose-dependent anti-inflammatory activity. At 20 mg/kg, significant edema reductions were observed at the 2nd ( = 0.035) and 3rd hours ( = 0.022), while at 40 mg/kg, reductions remained significant at the 2nd ( = 0.008) and 3rd hours ( = 0.046). Compound showed pronounced effects at 20 mg/kg at the 2nd ( = 0.005), 3rd ( < 0.001), and 4th hours ( = 0.004). Other compounds demonstrated minimal or no activity. Analgesic evaluation revealed that at 40 mg/kg, compound significantly reduced paw-licking time in the second phase ( = 0.038). Compounds , , and exhibited transient effects in the first phase only ( < 0.05). Compound lacked significant analgesic activity. The findings suggest that structural modifications may enhance efficacy for broader therapeutic applications.
腙以其C=N-NH官能团为特征，由于其与生物靶点相互作用的能力，在药物化学中是很有前景的候选物。本研究评估了-吡咯基碳酰肼（）和四种吡咯腙衍生物（）对雄性Wistar大鼠（6周龄）的抗炎和镇痛特性。使用角叉菜胶诱导的爪肿胀模型评估抗炎活性，而福尔马林、甩尾和爪退缩试验评估镇痛效果。化合物表现出剂量依赖性抗炎活性。在20mg/kg时，在第2小时（P = 0.035）和第3小时（P = 0.022）观察到显著的肿胀减轻，而在40mg/kg时，在第2小时（P = 0.008）和第3小时（P = 0.046）肿胀减轻仍显著。化合物在20mg/kg时在第2小时（P = 0.005）、第3小时（P < 0.001）和第4小时（P = 0.004）表现出明显效果。其他化合物表现出最小活性或无活性。镇痛评估显示，在40mg/kg时，化合物在第二阶段显著减少舔爪时间（P = 0.038）。化合物、和仅在第一阶段表现出短暂效果（P < 0.05）。化合物缺乏显著的镇痛活性。研究结果表明，结构修饰可能会提高疗效以用于更广泛的治疗应用。
