Identification of Indazole- and Azaindazole-Substituted Cyclopentapyrroles as G2019S Leucine-Rich Repeat Kinase 2 Inhibitors for the Treatment of CNS Disorders.

IF 4 3区 医学 Q2 CHEMISTRY, MEDICINAL ACS Medicinal Chemistry Letters Pub Date : 2025-02-13 eCollection Date: 2025-03-13 DOI:10.1021/acsmedchemlett.5c00045
Siyan Feng, Steven H Liang
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引用次数: 0

Abstract

This patent describes a novel class of novel indazole/azaindazole-substituted cyclopentapyrroles, which selectively inhibit the Leucine-Rich Repeat Kinase 2 (LRRK2) with G2019S mutation. These LRRK2 inhibitors are proposed for treating Parkinson's diseases, Alzheimer's disease, and other central nervous system (CNS) disorders.

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吲哚唑和叠氮唑取代环五吡咯作为G2019S富亮氨酸重复激酶2抑制剂治疗中枢神经系统疾病的鉴定
本专利描述了一类新型茚唑/氮杂唑取代环五吡咯,可选择性抑制G2019S突变的富亮氨酸重复激酶2 (LRRK2)。这些LRRK2抑制剂被建议用于治疗帕金森病、阿尔茨海默病和其他中枢神经系统(CNS)疾病。
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来源期刊
ACS Medicinal Chemistry Letters
ACS Medicinal Chemistry Letters CHEMISTRY, MEDICINAL-
CiteScore
7.30
自引率
2.40%
发文量
328
审稿时长
1 months
期刊介绍: ACS Medicinal Chemistry Letters is interested in receiving manuscripts that discuss various aspects of medicinal chemistry. The journal will publish studies that pertain to a broad range of subject matter, including compound design and optimization, biological evaluation, drug delivery, imaging agents, and pharmacology of both small and large bioactive molecules. Specific areas include but are not limited to: Identification, synthesis, and optimization of lead biologically active molecules and drugs (small molecules and biologics) Biological characterization of new molecular entities in the context of drug discovery Computational, cheminformatics, and structural studies for the identification or SAR analysis of bioactive molecules, ligands and their targets, etc. Novel and improved methodologies, including radiation biochemistry, with broad application to medicinal chemistry Discovery technologies for biologically active molecules from both synthetic and natural (plant and other) sources Pharmacokinetic/pharmacodynamic studies that address mechanisms underlying drug disposition and response Pharmacogenetic and pharmacogenomic studies used to enhance drug design and the translation of medicinal chemistry into the clinic Mechanistic drug metabolism and regulation of metabolic enzyme gene expression Chemistry patents relevant to the medicinal chemistry field.
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