著者
小林 義郎 田口 武夫
出版者
The Society of Synthetic Organic Chemistry, Japan
雑誌
有機合成化学協会誌 (ISSN:00379980)
巻号頁・発行日
vol.43, no.11, pp.1073-1082, 1985-11-01 (Released:2009-11-13)
参考文献数
70
被引用文献数
12 13

Studies on fluorine-modified vitamin D3 analogs : the design, synthesis and biological activity are reviewed. On the basis of the metabolism of vitamin D3 and the characteristic features of fluorine and fluorinated compounds, fluorine-modified vitamin D3 analogs were designed, synthesized and their biological activity was investigated to clarify the physiological significance of the metabolic hydroxylation of vitamin D3.
著者
赤羽 健司 上條 哲聖 飯塚 欣二 田口 武夫 小林 義郎 木曽 良明 梅山 秀明
出版者
The Pharmaceutical Society of Japan
雑誌
Chemical and Pharmaceutical Bulletin (ISSN:00092363)
巻号頁・発行日
vol.36, no.9, pp.3447-3452, 1988-09-25 (Released:2008-03-31)
参考文献数
31
被引用文献数
3 4

The structure-activity relationship of acyl-His-trifluorinated leucinol derivatives as inhibitors of human renal renin is discussed based upon the tertiary structure of human renin, which was deduced from the crystal structure of penicillopepsin by assuming structural similarity. The structural requirements for the inhibitors and possible interactions at the renin binding site are discussed.
著者
小林 義郎 熊懐 稜丸 田口 武夫
出版者
The Society of Synthetic Organic Chemistry, Japan
雑誌
有機合成化学協会誌 (ISSN:00379980)
巻号頁・発行日
vol.38, no.11, pp.1119-1129, 1980-11-01 (Released:2010-01-22)
参考文献数
36
被引用文献数
3 4

First, characteristics of a carbon-fluorine bond from the biological point of view are summarized with some examples : mimic effect, protective fluorination, irreversible conjugation with enzyme, increased lipophilicity and so on are presented. Secondly, some approaches to biologically active compounds utilizing the above characteristics are shown by the examples of trifluoromethylated nucleoside derivatives and fluorinated vitamin D3 analogues.