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

页码：2019 / 2026

页数：8

共 45 条

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