Diabetes is a disease linked to pathologies, such as chronic inflammation, neuropathy, and pain. The synthesis by the Claisen−Schmidt condensation reaction aims to obtain medium to high yield chalconic derivatives. Studies for the synthesis of new chalcone molecules aim at the structural manipulation of aromatic rings, as well as the replacement of rings by heterocycles, and combination through chemical reactions of synthesized structures with other molecules, in order to enhance biological activity. A chalcone was synthesized and evaluated for its antinociceptive, anti-inflammatory and hypoglycemic effect in adult zebrafish. In addition to reducing nociceptive behavior, chalcone (40 mg/kg) reversed post-treatment-induced acute and chronic hyperglycemia and reduced carrageenan-induced abdominal edema in zebrafish. It also showed an inhibitory effect on NO production in J774A.1 cells. When compared with the control groups, the oxidative stress generated after chronic hyperglycemia and after induction of abdominal edema was significantly reduced by chalcone. Molecular docking simulations of chalcone with Cox -1, Cox-2, and TRPA1 channel enzymes were performed and indicated that chalcone has a higher affinity for the COX-1 enzyme and 4 interactions with the TRPA1 channel. Chalcone also showed good pharmacokinetic properties as assessed by ADMET.

糖尿病是一种与慢性炎症、神经病变和疼痛等病理相关的疾病。通过克莱森-施密特缩合反应合成的目的是获得中高产率的查尔酮衍生物。新型查尔酮分子的合成研究旨在对芳香环进行结构操控，以及用杂环取代环，并通过合成结构与其他分子的化学反应进行结合，以增强生物活性。合成了一种查耳酮，并评估了其对成年斑马鱼的镇痛、抗炎和降血糖作用。除了减少伤害性行为外，查尔酮（40 毫克/千克）还可以逆转治疗后引起的急性和慢性高血糖，并减少角叉菜胶引起的斑马鱼腹部水肿。它还显示出对 J774A.1 细胞中 NO 产生的抑制作用。与对照组相比，查尔酮显着降低了慢性高血糖和诱导腹部水肿后产生的氧化应激。对查耳酮与Cox -1、Cox-2和TRPA1通道酶进行分子对接模拟，结果表明查尔酮对COX-1酶具有较高的亲和力，并且与TRPA1通道有4种相互作用。通过 ADMET 评估，查耳酮还显示出良好的药代动力学特性。