期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 8, 期 6, 页码 1245-1252出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0968-0896(00)00076-6
关键词
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The synthesis of a new series of P450 17 inhibitors is described. The imidazol-1-yl compounds 5 showed strong inhibition of P450 17 rat and especially human enzyme, the most active compounds being 5ax, 5ay and 5bx with IC50 values of 0.17, 0.24 and 0.25 mu M respectively (ketoconazole: 0.74 mu M). The 1,2,4-triazol-1-yl compounds 6 were less active, while the 1,2,4-triazol-4-yl compounds 7 were inactive. The title compounds showed little inhibition of P450 arom. The most active P450 17 inhibitors 5ax and 5ay markedly decreased the testosterone plasma concentration of SD rats 2 h after application of 0.019 mmol/kg. After 6 h, 5ay still exhibited a strong effect. (C) 2000 Elsevier Science Ltd. All rights reserved.
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