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研究生:陳文雄
研究生(外文):Chen, Wen Shiung
論文名稱:1,4-benzodiazepine-2,5-dione之合成研究
論文名稱(外文):The synthetic studies of 1,4-benzodiazepine-2,5-dione
指導教授:何東英何東英引用關係
指導教授(外文):He, Dong-Ying
學位類別:碩士
校院名稱:國立臺灣大學
系所名稱:化學研究所
學門:自然科學學門
學類:化學學類
論文種類:學術論文
論文出版年:1997
畢業學年度:85
語文別:中文
論文頁數:94
中文關鍵詞:內皮素拮抗劑化學工程化學
外文關鍵詞:Endothelin receptor antagonistCHEMICAL-ENGINEERINGCHEMISTRY
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Endothelin-1 (ET-1), a 38 amino acid peptide, isolated from endothelial
cells of cardiovascular system has been identified as one of the most potent
constrictors of human vesels In the search of endothelin receptor antagonists
as potential anti-hypertensive agents, extensive efforts have been
accomplished.
Based on NMR derived structure of ET-1, SB 209670,a highly potent
endothelin receptor antagonist was designed. The 1- and 3-phenyl groups are
used as mimic of the aromatic side chains of Tyr-13 and Phe-14 of ET-1.
The 2-carboxylic acid of SB 209670 was designed to mimic the Asp-18 of
ET-1. Our interested compound 4-N-phenyl-1,4-benzodiazepine-2,5-dione are
derived from structural modification of compound SB 209670 by computer aided
molecular modeling using commercial available software. A number of approaches
to this ring system have been described in the literature,now we suggest an
another efficient way to synthesize a variety of 4-N-benzenoid-substituted
analogs of 1,4-benzodiazepine-2,5-dione .

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