Ergena Asrat, Rajeshwar Yerra, Solomon Gebremedhin
Department of Pharmaceutical Chemistry, College of Medicine and Health Sciences, University of Gondar, Gondar, Ethiopia.
Department of Medicinal Chemistry, College of Health Sciences, Mekelle University, Mekelle, Ethiopia.
Scientifica (Cairo). 2022 Apr 8;2022:3011531. doi: 10.1155/2022/3011531. eCollection 2022.
1,3,4-Thiadiazole nuclease, a 5-membered heterocyclic ring system containing two nitrogen and one sulfur atoms in addition to carbon atoms, is compound that showed promising results in the process of searching new diuretic agents. In this study, seven 5- and 2-thioate derivatives of 1, 3, 4-thiadiazoles were synthesized by substitution reaction using acetone as solvent and KCO as a base. The compounds ware then characterized by using IR and NMR spectroscopy. The diuretic activity of the compounds was evaluated on Swiss albino mice by measuring urine volume, urinary pH, and urinary Na, K, and Cl. The result showed increase in urinary excretion of both water and electrolytes. 5-Methyl-substituted derivatives of 1, 3, 4-thiadiazoles showed significant increase in excretion of both water and electrolytes when they are compared to both negative control and 5-amino-substituted derivatives. The highest diuretic activity (0.82) was recorded for para-nitro-substituted benzene ring at 2-thioate group of 5-methyl-1, 3, 4-thiadiazole, while the least (0.56) was recorded for propanethioate group at 2 position and amine group at 5 position of 1, 3, 4-thiadiazole. The finding of the present study showed that all the compounds have diuretic activity and 5-methyl derivatives of 1, 3, 4-thiadiazoles exhibited significant diuretic activity.
1,3,4-噻二唑核酸酶是一种除碳原子外还含有两个氮原子和一个硫原子的五元杂环系统化合物，在寻找新型利尿剂的过程中显示出了有前景的结果。在本研究中，以丙酮为溶剂、碳酸钾为碱，通过取代反应合成了七种1,3,4-噻二唑的5-和2-硫代酸酯衍生物。然后利用红外光谱和核磁共振光谱对这些化合物进行了表征。通过测量尿量、尿pH值以及尿钠、钾和氯，在瑞士白化小鼠身上评估了这些化合物的利尿活性。结果表明水和电解质的尿排泄量增加。与阴性对照和5-氨基取代衍生物相比，1,3,4-噻二唑的5-甲基取代衍生物在水和电解质排泄方面均有显著增加。在5-甲基-1,3,4-噻二唑的2-硫代酸酯基团的对硝基取代苯环处记录到最高利尿活性（0.82），而在1,3,4-噻二唑的2位丙硫代酸酯基团和5位胺基团处记录到最低利尿活性（0.56）。本研究结果表明所有化合物均具有利尿活性，且1,3,4-噻二唑的5-甲基衍生物表现出显著的利尿活性。
