頁籤選單縮合
題名 | Studies on Quinazlines X. Synthesis and Pharmacological Evaluation of 4(3H)-Quinazolinone Biphenyl Tetrazoles as Angiotensin Ⅱ Antagonists= |
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作者 | 陳基旺; 羅吉鈞; 林華美; 鄭逢吉; Chern, Ji-wang; Lo, Jir-chun; Lin, Hua-mei; Cheng, Fong-chi; Usifoh,Cyril O.; |
期刊 | 中華藥學雜誌 |
出版日期 | 19990200 |
卷期 | 51:1 1999.02[民88.02] |
頁次 | 頁31-48 |
分類號 | 418.1 |
語文 | eng |
關鍵詞 | Quinazolinone; Biphenyl tetrazole; Angiotensin Ⅱ antagonist; |
英文摘要 | A series of 2-substituted 3- [[2- (tetrazol-5-yl)biphenyl-4-yl]methyl]qulna-zolin-4(3H)-ones (3a-h) were synthesized as potential angiotensin II antagonists. Compounds with 2-carboxylic acid (3a), 2-ethoxycarbonyl (3b), 2-carboxamide (3c), 2-phenyl (3d), 2-propionic acid (3e), 2-butyric acid (30, 2-pentanone (3g), 2-benzyl (3h) were selected for study. A preliminary assay of compounds 3a-f,h against the angiotensin AT□ receptor revealed weak activity with IC□ values In the μM range. They also displayed lower affinity for the AT□ receptor than for the AT□ receptor. However, compounds with lipophilic or hydrophobic substituents such as 3b,d displayed better affinity to ATi receptors than compounds with polar or hydrophilic substituents such as 3b-c,e-f. Among this series of compounds, compound 3b was most active against the ATi receptor with an IC□ value of 0.56μM. |
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