| 张龙,张敏杰,陈娅芳,张艳,於祥.化学通报,2025,88(4):437-442. |
| 含1,3,4-噁二唑的petibirin A类似物利尿排石活性研究 |
| Diuretic and Litholytic Activities of Petibirin A Analogues Containing 1,3,4-Oxadiazole |
| 投稿时间：2024-12-06 修订日期：2025-01-05 |
| DOI： |
| 中文关键词: 尿石症 petibirin A 1,3,4-噁二唑 利尿排石 分子对接 |
| 英文关键词:Urolithiasis Petibirin A 1,3,4-Oxadiazole Diuretic and litholytic activity Molecular docking |
| 基金项目:贵州省科技计划项目(黔科合基础-ZK[2022]一般503和黔科合基础-ZK[2023]一般426)资助 |
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| 中文摘要: |
| 对前期合成的54个含1,3,4-噁二唑的petibirin A类似物进行利尿排石活性研究。采用犬肾小管上皮细胞MDCK进行体外利尿排石活性评价。结果显示化合物D4具有显著的利尿排石活性，且对MDCK细胞无显著毒性。可作为利尿排石候选药物。分子对接结果表明，化合物D4可以和利尿调节关键蛋白赖氨酸蛋白缺乏激酶1（WNK1）显著结合。 |
| 英文摘要: |
| 54 petibirin A analogues containing 1,3,4-oxadiazole synthesized in the early stage were studied on the diuretic and litholytic activity in vitro using canine renal tubular epithelial cell MDCK. The results showed that compound D4 exhibited significant diuretic and litholytic activities, and had no significant toxicity to MDCK cells, which could be further developed into novel diuretic agents. The molecular docking results showed that compound D4 could significantly bind to the key diuretic regulatory protein WNK1. |
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