{"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":"<p><p>A series of novel oxadiazole derivatives were designed, synthesized, and evaluated for their pharmacological effects. All target compounds were subjected to analysis using <sup>1</sup>H NMR, <sup>13</sup>C 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 <b>IV</b><sub><b>1</b></sub> and <b>IV</b><sub><b>2</b></sub> were particularly effective, demonstrating comparable or greater potency in reducing blood pressure compared to Losartan. Therefore, compounds <b>IV</b><sub><b>1</b></sub> and <b>IV</b><sub><b>2</b></sub> have the potential to be developed as antihypertension medications.</p>","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\":\"<p><p>A series of novel oxadiazole derivatives were designed, synthesized, and evaluated for their pharmacological effects. All target compounds were subjected to analysis using <sup>1</sup>H NMR, <sup>13</sup>C 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 <b>IV</b><sub><b>1</b></sub> and <b>IV</b><sub><b>2</b></sub> were particularly effective, demonstrating comparable or greater potency in reducing blood pressure compared to Losartan. Therefore, compounds <b>IV</b><sub><b>1</b></sub> and <b>IV</b><sub><b>2</b></sub> have the potential to be developed as antihypertension medications.</p>\",\"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}
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.
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.
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