Lahti R A, Gall M
J Med Chem. 1976 Aug;19(8):1064-7. doi: 10.1021/jm00230a017.
The results of this study suggest that 5-chloro-2-[3-methyl-5-(dimethylamino)methyltriazol-4-yl]benzophenone can undergo N-dealkylation and ring closure in vivo to form the corresponding benzodiazepine. The in vivo conversion was found to occur in mice, rats, and monkeys. A variety of substituted aminobenzophenone compounds were also able to undergo these conversions. The conversions to benzodiazepines were confirmed by a comparison of retention times on a gas chromatograph as well as through the use of a GC-mass spectrometer. The results obtained did not prove that the N-alkylaminobenzophenones were devoid of activity, but they do suggest that their observed pharmacological activity may be due to the formation of the corresponding benzodiazepines.
本研究结果表明，5-氯-2-[3-甲基-5-(二甲基氨基)甲基三唑-4-基]二苯甲酮在体内可发生N-脱烷基化和环化反应，形成相应的苯二氮䓬类化合物。体内转化在小鼠、大鼠和猴子中均有发现。多种取代氨基二苯甲酮化合物也能够发生这些转化。通过比较气相色谱上的保留时间以及使用气相色谱-质谱联用仪，证实了向苯二氮䓬类化合物的转化。所获得的结果并未证明N-烷基氨基二苯甲酮没有活性，但确实表明它们所观察到的药理活性可能是由于相应苯二氮䓬类化合物的形成。
