A simple, efficient, and straightforward one‐pot three‐component synthesis of functionalized tetrahydropyrans (6a‐l) is carried‐out in the presence of an inexpensive and environmentally benign Eaton's reagent as a catalyst to discover some ACE inhibitors and anti‐inflammatory agents. Angiotensin‐converting enzyme (ACE) is highly involved in the renin‐angiotensin system and often directly associated with cardiovascular dysfunction via inflammation. Thus, the cardiovascular protective effect of newly synthesized tetrahydropyrans (6a‐l) was evaluated through ACE inhibition, human red blood cell (HRBC) membrane stabilization, and molecular docking studies. As the results complied, compounds 6e and 6f were identified as effective ACE inhibitors. Docking studies, HRBC based anti‐inflammatory assay, and SAR studies revealed that compounds 6e and 6f could be good anti‐inflammatory agents apart from ACE inhibitors.

中文翻译：

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改进的多组分一锅法合成功能化四氢吡喃心血管功能障碍调节剂

在廉价且环保的伊顿试剂作为催化剂的情况下，进行简单，高效，直接的一锅三组分官能化四氢吡喃（6a-1）合成实验，以发现一些ACE抑制剂和抗炎药。血管紧张素转换酶（ACE）高度参与肾素-血管紧张素系统，通常通过炎症与心血管功能障碍直接相关。因此，通过ACE抑制，人类红细胞（HRBC）膜稳定和分子对接研究评估了新合成的四氢吡喃（6a-1）对心血管的保护作用。结果符合，化合物6e和6f被确定为有效的ACE抑制剂。对接研究，基于HRBC的抗炎测定以及SAR研究表明，化合物6e和6f除了是ACE抑制剂以外，可能是良好的抗炎药。