新型强效人神经肽Y-Y5受体拮抗剂。第4部分：四氢二氮杂苯并薁衍生物。
Novel potent antagonists of human neuropeptide Y-Y5 receptor. Part 4: tetrahydrodiazabenzazulene derivatives.
作者信息
Satoh Yoshinari, Hatori Chie, Ito Harunobu
机构信息
Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan.
出版信息
Bioorg Med Chem Lett. 2002 Apr 8;12(7):1009-11. doi: 10.1016/s0960-894x(02)00090-2.
Novel tetrahydrodiazabenzazulene derivatives, designed from the lead compound 1 discovered by screening of our in-house chemical library, were prepared and found to be potent neuropeptide Y-Y5 (NPY-Y5) receptor antagonists. The structure-activity relationships are described. Compounds 7 (FR240662) and 16 (FR252384) were especially attractive owing to their high affinities for the NPY-Y5 receptors, oral absorption and permeability to brain.
从我们内部化学文库筛选出的先导化合物1设计合成了新型四氢二氮杂苯并薁衍生物，发现它们是有效的神经肽Y-Y5（NPY-Y5）受体拮抗剂。描述了构效关系。化合物7（FR240662）和16（FR252384）因其对NPY-Y5受体的高亲和力、口服吸收性和脑通透性而特别引人注目。
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