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 <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.
Authors
- Lan-ling Zhang
- Xiang Lian (ORCID: https://orcid.org/0000-0002-9375-9862)
- Zhuo Wu (ORCID: https://orcid.org/0000-0002-2654-5362)
- Zheng Qu
- Xu Wang (ORCID: https://orcid.org/0009-0004-6052-9130)
Institutions
- Shanghai Institute of Technology (CN)
Publication Details
- Journal
- Chemical Research in Toxicology
- Published
- 2024-12-13
- DOI
- https://doi.org/10.1021/acs.chemrestox.4c00368
- Citations
- 2
- Primary Topic
- Computational Drug Discovery Methods
- Type
- article
- Field-Weighted Citation Impact
- 0.72
Funders
- Shanghai Municipal Education Commission