Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.
Department of Pharmacology & Toxicology, Faculty of Pharmacy, Minia University, El-Minia 61519, Egypt.
Future Med Chem. 2020 Jan;12(1):37-50. doi: 10.4155/fmc-2019-0160. Epub 2019 Nov 11.
Hypertension is a major health problem worldwide resulting in high death rates due to its consequences and complications. Therefore, searching for new vasorelaxants is a must to find new vasodilators efficient for the treatment of different cardiovascular diseases. Different 6-phenyl-3-pyridazinone based derivatives were synthesized and screened for their vasorelaxant activity according to the reported method using hydralazine as a standard. The tested compounds revealed potent to mild activity with EC values 0.339-114.300 μM compared with hydralazine EC = 18.210 μM. The most active compounds were the acid , its ester analog and 4-methoxyphenylhydrazide derivative (EC = 0.339, 1.225 and 1.204 μM, respectively). Therefore, 6-phenylpyridazin-3(2)-one can be a hit for structural optimization to obtain promising vasorelaxants.
高血压是全球范围内的一个主要健康问题，由于其后果和并发症，导致死亡率很高。因此，寻找新的血管舒张剂是必须的，以寻找治疗不同心血管疾病的有效新血管扩张剂。根据报道的方法，用肼屈嗪作为标准，合成了不同的 6-苯基-3-哒嗪酮基衍生物，并对其血管舒张活性进行了筛选。与肼屈嗪 EC = 18.210 μM 相比，测试化合物的 EC 值为 0.339-114.300 μM，具有有效至轻度的活性。最活跃的化合物是酸、其酯类似物和 4-甲氧基苯肼衍生物（EC 值分别为 0.339、1.225 和 1.204 μM）。因此，6-苯基哒嗪-3（2）-酮可以作为结构优化的起点，以获得有前途的血管舒张剂。
