{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,12,31]],"date-time":"2025-12-31T17:53:15Z","timestamp":1767203595457,"version":"build-2238731810"},"reference-count":23,"publisher":"MDPI AG","issue":"11","license":[{"start":{"date-parts":[[2017,11,3]],"date-time":"2017-11-03T00:00:00Z","timestamp":1509667200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"content-domain":{"domain":["www.mdpi.com"],"crossmark-restriction":true},"short-container-title":["Molecules"],"abstract":"<jats:p>Under the guidance of combination of traditional Chinese medicine chemistry (CTCMC), this study describes the preparation of a phenolic acid\/dipeptide\/borneol hybrid consisting of phenolic acid and a bornyl moiety connected to the dipeptide N-terminal and C-terminal respectively. It also evaluates their angiotensin converting enzyme (ACE) inhibitory and synergistic antihypertensive activities. Briefly, a series of novel phenolic acid\/dipeptide\/borneol hybrids were prepared and investigated for their ability to inhibit ACE. The influence of the phenolic acid and bornyl moiety on subsite selectivity is also demonstrated. Among all the new compounds, two compounds\u20147a and 7g\u2014reveal good inhibition potency in in vitro ACE-inhibitory tests. Interestingly, favorable binding results in molecular docking studies also supported the in vitro results. Additionally, the bioassay showed that oral administration of the two compounds displayed high and long-lasting antihypertensive activity both in acute antihypertensive tests and in therapeutic antihypertensive tests by non-invasive blood pressure measurements in spontaneously hypertensive rats.<\/jats:p>","DOI":"10.3390\/molecules22111739","type":"journal-article","created":{"date-parts":[[2017,11,3]],"date-time":"2017-11-03T12:39:20Z","timestamp":1509712760000},"page":"1739","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":10,"title":["Design, Synthesis, and Evaluation of Novel Phenolic Acid\/Dipeptide\/Borneol Hybrids as Potent Angiotensin Converting Enzyme (ACE) Inhibitors with Anti-hypertension Activity"],"prefix":"10.3390","volume":"22","author":[{"given":"Ying","family":"Sun","sequence":"first","affiliation":[{"name":"Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Northwest University, Xi\u2019an 710069, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yujun","family":"Bai","sequence":"additional","affiliation":[{"name":"Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Northwest University, Xi\u2019an 710069, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Xirui","family":"He","sequence":"additional","affiliation":[{"name":"Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Northwest University, Xi\u2019an 710069, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yajun","family":"Bai","sequence":"additional","affiliation":[{"name":"Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Northwest University, Xi\u2019an 710069, China"},{"name":"Key Laboratory of Synthetic and Natural Functional Molecule Chemistry of the Ministry of Education, College of Chemistry &amp; Materials Science, Northwest University, Xi\u2019an 710127, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Pei","family":"Liu","sequence":"additional","affiliation":[{"name":"Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Northwest University, Xi\u2019an 710069, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Zefeng","family":"Zhao","sequence":"additional","affiliation":[{"name":"Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Northwest University, Xi\u2019an 710069, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Xufei","family":"Chen","sequence":"additional","affiliation":[{"name":"Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Northwest University, Xi\u2019an 710069, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Xiaohui","family":"Zheng","sequence":"additional","affiliation":[{"name":"Key Laboratory of Resource Biology and Biotechnology in Western China, Ministry of Education, Northwest University, Xi\u2019an 710069, China"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2017,11,3]]},"reference":[{"key":"ref_1","first-page":"3062","article-title":"Hypertension as a part of metabolic cardiovascular syndrome","volume":"111","author":"Os","year":"1991","journal-title":"Tidsskr. 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