Scaffold hopping of fused piperidine-type NK3 receptor antagonists to reduce environmental impact

被引：1
|
作者：
Yamamoto, Koki [1 ]
Inuki, Shinsuke [1 ]
Ohno, Hiroaki [1 ]
Oishi, Shinya [1 ]
机构：
[1] Kyoto Univ, Grad Sch Pharmaceut Sci, Sakyo Ku, Kyoto 6068501, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY | 2019年 / 27卷 / 10期
关键词：
Environmental impact; Fezolinetant; GnRH; NK3; receptor; Scaffold hopping; WATER TREATMENT-PLANT; HUMAN NEUROKININ-3 RECEPTOR; PHARMACEUTICALS; KISSPEPTIN; SECRETION; HORMONES; FATE; GNRH; PHOTODEGRADATION; IDENTIFICATION;
D O I：
10.1016/j.bmc.2019.03.059
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Neurokinin-3 receptor (NK3R) plays a pivotal role in the release of gonadotropin-releasing hormone in the hypothalamus-pituitary-gonadal (HPG) axis. To develop novel NK3R antagonists with less environmental toxicity, a series of heterocyclic scaffolds for the triazolopiperazine substructure in an NK3R antagonist fezoli-netant were designed and synthesized. An isoxazolo[3,4-c]piperidine derivative exhibited moderate NK3R antagonistic activity and favorable properties that were decomposable under environmental conditions.
引用
收藏
页码：2019 / 2026
页数：8
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