环状 GMP-AMP 合成酶 (cGAS) 抑制剂是治疗自身免疫性疾病和炎症性疾病的潜在药物

IF 4 3区医学 Q2 CHEMISTRY, MEDICINAL

ACS Medicinal Chemistry Letters Pub Date : 2024-08-22 DOI:10.1021/acsmedchemlett.4c0039210.1021/acsmedchemlett.4c00392

Ahmed F. Abdel-Magid*,

引用次数: 0

摘要

本专利申请中的发明涉及大环苯并咪唑衍生物，一般由式 1 表示。式 1 的化合物是 cGAS 抑制剂，可用于治疗系统性红斑狼疮、系统性硬化症（SSc）、干扰素病等自身免疫性疾病。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Inhibitors of the Cyclic GMP-AMP Synthase (cGAS) as Potential Treatment for Autoimmune and Inflammatory Diseases

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Inhibitors of the Cyclic GMP-AMP Synthase (cGAS) as Potential Treatment for Autoimmune and Inflammatory Diseases

The invention in this patent application relates to macrocyclic benzimidazole derivatives represented herein generally by Formula 1. The compounds of Formula 1 are cGAS inhibitors and may potentially provide treatments of autoimmune diseases such as systemic lupus erythematosus, systemic sclerosis (SSc), interferonopathies, and others.

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来源期刊

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.