ドラッグ・デザインとしてのビタミン新誘導体

概要

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It has been concluded in the previous discussion on modified thiamine compounds ^<7>)that any modification of the thiamine molecule will cause loss of activity, unless the modified compounds can be reverted to thiamine in vivo. The similar conclusion will be applied to any modification of vitamins ; their vitamin activity can be expected only when the modified derivatives will be easily converted to the original vitamins in animal or human metabolism. Successful design of new vitamin derivatives as drugs will be differentiated into two directions : 1) More stabilized and easily absorbable modification of vitamins as effective vitamin preparations, 2) more specific and non-revertible modification of vitamins as antivitamins or permanently altered compounds as pharmacological agents. It is necessary to evaluate modified compounds of vitamins from the standpoints of rational development and application of drugs. Misbranded use of modified thiamine compounds such as "acrtive vitamin B_1 preparations" or exaggerated effectiveness should be strictly controlled thru rational evaluation of each modified compound.
日本ビタミン学会の論文
1971-02-25