作为糖苷酶和HIV/FIV蛋白酶抑制剂的C2对称四羟基氮杂环庚烷
C2-symmetrical tetrahydroxyazepanes as inhibitors of glycosidases and HIV/FIV proteases.
作者信息
Qian X, Morís-Varas F, Fitzgerald M C, Wong C H
机构信息
Department of Chemistry, Scripps Research Institute, La Jolla, CA 92037, USA.
出版信息
Bioorg Med Chem. 1996 Dec;4(12):2055-69. doi: 10.1016/s0968-0896(96)00218-0.
C2-Symmetrical tetrahydroxyazepanes were synthesized as inhibitors for glycosidases. Tetrahydroxyazepane 1 is a non-specific inhibitor of various glycosidases, while compounds 2, 3 and 4 specifically inhibit beta-N-acetylglucosaminidase, beta-glucosidase, and alpha-fucosidase, respectively, with Ki in the micromolar range. Compound 1 is not an inhibitor of HIV/FIV proteases, but its 3,6-difluorobenzyl derivatives are moderate inhibitors of both enzymes.
合成了C2对称的四羟基氮杂环庚烷作为糖苷酶抑制剂。四羟基氮杂环庚烷1是多种糖苷酶的非特异性抑制剂，而化合物2、3和4分别特异性抑制β-N-乙酰氨基葡萄糖苷酶、β-葡萄糖苷酶和α-岩藻糖苷酶，其抑制常数（Ki）在微摩尔范围内。化合物1不是HIV/FIV蛋白酶的抑制剂，但其3,6-二氟苄基衍生物是这两种酶的中度抑制剂。
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