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Synthesis and the Investigation of the Novel Structure-activity Relationship of the Rennin Inhibitor

Author: XieJiaRong
Tutor: CaiLiangZhen；XieJianShu
School: East China University of Science and Technology
Course: Pharmaceutical Engineering
Keywords: Renin inhibitor Synthesis Hypertension rennin-angiotensin system
CLC: TQ467
Type: Master's thesis
Year: 2011
Downloads: 87
Quote: 0
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Abstract


Hypertension is a major risk factor for cardiovascular diseases such as stroke, myocardial infarction. The rennin-angiotensin system (RAS) is widely accepted as a major regulator of cardiovascular and renal function, and plays a major role in water and salt homeostasis, as well as blood pressure control. Aliskiren as a novel orally effective rennin inhibitor, can prevent the formation of Ang I and Ang II, and is effective for the treatment of hypertension and related cardiovascular diseases.For the purpose of getting some better compounds, I begin with my graduate program after searching many literatures, and patents on the base of ours hit and compute analysis. According to the principle of pharmaceutical chemistry and structure-based drug design, we independently design and synthesize many compounds which contain so different molecule framework such as biphenyls and substituted morpholines. Most of them are new compounds which aren’t synthesized by others. And in some steps, we apply some new ways of synthesis. Although the yield is no high, they can be gotten with complex structure. All of these synthesized compounds are given the results of the test of their biological activity in vitro. The result indicates that the compounds of biphenyls have the inhibiting activity whose the value of IC50 is from 10-6 M to 10"8M. And the result is related with the site of biphenyl and the substituted group. The IC50 of other compounds with methyl quinoline is from 10-7 to 10-9, better than those no methyl group. Most of them have good results. The most potent inhibitor is the compound with an IC50 of 9 nM and has been on the way of biological activity test in vivo.On the base of investigating the structure-activity relationship (SAR), we can conclude that the rule of SAR that will provide some useful help for the subsequent research and find some compounds with better activities.

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