新型恶二唑类高效降压药的设计、合成及生物学评价。

IF 3.7 3区医学 Q2 CHEMISTRY, MEDICINAL

Chemical Research in Toxicology Pub Date : 2025-01-20 Epub Date: 2024-12-12 DOI:10.1021/acs.chemrestox.4c00368

Zheng Qu, Xu Wang, Lan-Ling Zhang, Xiang Lian, Zhuo Wu

{"title":"新型恶二唑类高效降压药的设计、合成及生物学评价。","authors":"Zheng Qu, Xu Wang, Lan-Ling Zhang, Xiang Lian, Zhuo Wu","doi":"10.1021/acs.chemrestox.4c00368","DOIUrl":null,"url":null,"abstract":"A series of novel oxadiazole derivatives were designed, synthesized, and evaluated for their pharmacological effects. All target compounds were subjected to analysis using 1H NMR, 13C NMR, and mass spectrometry. They showed a strong affinity to the AT1 receptor and effectively lowered blood pressure in spontaneously hypertensive rats at a nanomolar level. Compounds IV1 and IV2 were particularly effective, demonstrating comparable or greater potency in reducing blood pressure compared to Losartan. Therefore, compounds IV1 and IV2 have the potential to be developed as antihypertension medications.","PeriodicalId":31,"journal":{"name":"Chemical Research in Toxicology","volume":" ","pages":"145-150"},"PeriodicalIF":3.7000,"publicationDate":"2025-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Design, Synthesis, and Biological Evaluation of New Oxadiazole Derivatives as Efficient Antihypertension Drugs.\",\"authors\":\"Zheng Qu, Xu Wang, Lan-Ling Zhang, Xiang Lian, Zhuo Wu\",\"doi\":\"10.1021/acs.chemrestox.4c00368\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"A series of novel oxadiazole derivatives were designed, synthesized, and evaluated for their pharmacological effects. All target compounds were subjected to analysis using 1H NMR, 13C NMR, and mass spectrometry. They showed a strong affinity to the AT1 receptor and effectively lowered blood pressure in spontaneously hypertensive rats at a nanomolar level. Compounds IV1 and IV2 were particularly effective, demonstrating comparable or greater potency in reducing blood pressure compared to Losartan. Therefore, compounds IV1 and IV2 have the potential to be developed as antihypertension medications.\",\"PeriodicalId\":31,\"journal\":{\"name\":\"Chemical Research in Toxicology\",\"volume\":\" \",\"pages\":\"145-150\"},\"PeriodicalIF\":3.7000,\"publicationDate\":\"2025-01-20\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Chemical Research in Toxicology\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1021/acs.chemrestox.4c00368\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/12/12 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Chemical Research in Toxicology","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1021/acs.chemrestox.4c00368","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/12/12 0:00:00","PubModel":"Epub","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}

引用次数: 0

摘要

研究人员设计、合成了一系列新型噁二唑衍生物，并对其药理作用进行了评估。对所有目标化合物都进行了 1H NMR、13C NMR 和质谱分析。这些化合物与 AT1 受体有很强的亲和力，能在纳摩尔水平上有效降低自发性高血压大鼠的血压。化合物 IV1 和 IV2 尤其有效，与洛沙坦相比，它们的降压效果相当或更强。因此，化合物 IV1 和 IV2 有潜力开发成抗高血压药物。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

查看原文本刊更多论文

Design, Synthesis, and Biological Evaluation of New Oxadiazole Derivatives as Efficient Antihypertension Drugs.

A series of novel oxadiazole derivatives were designed, synthesized, and evaluated for their pharmacological effects. All target compounds were subjected to analysis using ¹H NMR, ¹³C NMR, and mass spectrometry. They showed a strong affinity to the AT1 receptor and effectively lowered blood pressure in spontaneously hypertensive rats at a nanomolar level. Compounds IV₁ and IV₂ were particularly effective, demonstrating comparable or greater potency in reducing blood pressure compared to Losartan. Therefore, compounds IV₁ and IV₂ have the potential to be developed as antihypertension medications.

求助全文

通过发布文献求助，成功后即可免费获取论文全文。去求助

来源期刊

Chemical Research in Toxicology 医学-毒理学

CiteScore

7.90

自引率

7.30%

发文量

215

审稿时长

3.5 months

期刊介绍： Chemical Research in Toxicology publishes Articles, Rapid Reports, Chemical Profiles, Reviews, Perspectives, Letters to the Editor, and ToxWatch on a wide range of topics in Toxicology that inform a chemical and molecular understanding and capacity to predict biological outcomes on the basis of structures and processes. The overarching goal of activities reported in the Journal are to provide knowledge and innovative approaches needed to promote intelligent solutions for human safety and ecosystem preservation. The journal emphasizes insight concerning mechanisms of toxicity over phenomenological observations. It upholds rigorous chemical, physical and mathematical standards for characterization and application of modern techniques.