新型3-磺酰基-8-氮杂双环[3.2.1]辛烷类长链脂肪酸延长酶6（ELOVL6）抑制剂的合成与生物学评价
Synthesis and biological evaluation of a novel 3-sulfonyl-8-azabicyclo[3.2.1]octane class of long chain fatty acid elongase 6 (ELOVL6) inhibitors.
作者信息
Nagase Tsuyoshi, Takahashi Toshiyuki, Sasaki Takahide, Nagumo Akira, Shimamura Ken, Miyamoto Yasuhisa, Kitazawa Hidefumi, Kanesaka Maki, Yoshimoto Ryo, Aragane Katsumi, Tokita Shigeru, Sato Nagaaki
机构信息
Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co, Ltd, Tsukuba, Ibaraki 300-2611, Japan.
出版信息
J Med Chem. 2009 Jul 23;52(14):4111-4. doi: 10.1021/jm900488k.
Long chain fatty acid elongase 6 (ELOVL6) catalyzes the elongation of long chain fatty acyl-CoAs and is a potential target for the treatment of metabolic disorders. The ultrahigh throughput screen of our corporate chemical collections resulted in the identification of a novel 3-sulfonyl-8-azabicyclo[3.2.1]octane class of ELOVL6 inhibitor 1a. Optimization of lead 1a led to the identification of the potent, selective, and orally available ELOVL6 inhibitor 1w.
长链脂肪酸延长酶6（ELOVL6）催化长链脂肪酰辅酶A的延长，是治疗代谢紊乱的潜在靶点。对我们公司化学库的超高通量筛选鉴定出了一种新型的3-磺酰基-8-氮杂双环[3.2.1]辛烷类ELOVL6抑制剂1a。对先导化合物1a进行优化后鉴定出了强效、选择性且口服有效的ELOVL6抑制剂1w。
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