有機合成化学協会誌
Online ISSN : 1883-6526
Print ISSN : 0037-9980
ISSN-L : 0037-9980
総説および総合論文
活性型ビタミンD誘導体の創薬研究と実用的合成法
久保寺 登
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2010 年 68 巻 9 号 p. 904-910

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In vitamin D research, there have been three milestones from the perspective of pharmaceutical studies. The first was the early stages of vitamin D research and involved the discovery of vitamin D and its physiological significance as an anti-rickets factor. The second was the elucidation of the vitamin D activation pathway in the body and the discovery of biologically active metabolites. The third has been characterized by the discovery of the differentiation-inducing properties of active vitamin D. This indicated the diversity of the physiological actions of active vitamin D, which initially had been thought only to contribute to bone and calcium metabolism. Because these physiological actions were clinically useful, the third discovery revealed opportunities for the development of drugs appropriate to specific purposes by synthesizing derivatives to separate biological effects. Six active vitamin D derivatives (maxacalcitol, calcipotriol, tacalcitol, paricalcitol, doxercalciferol, and falecalcitriol) based on the findings during the third milestone are now commercially available and contributing to current clinical practice. This article discusses the various milestones outlining vitamin D and derivatives in terms of pharmaceutical studies and practical syntheses of the six derivatives developed during the third milestone.

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© 2010 社団法人 有機合成化学協会
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