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新型苯并呋喃-吡唑-吡啶类分子用于骨关节炎治疗的开发。

Development of a New Benzofuran-Pyrazole-Pyridine-Based Molecule for the Management of Osteoarthritis.

机构信息

Department of Therapeutic Chemistry, Pharmaceutical and Drug Industries Research Institute, National Research Centre (NRC), El Bohouth St., Dokki, Cairo 12622, Egypt.

Department of Pathology, Faculty of Veterinary Medicine, Cairo University, Cairo 12211, Egypt.

出版信息

Molecules. 2023 Sep 27;28(19):6814. doi: 10.3390/molecules28196814.

DOI:10.3390/molecules28196814
PMID:37836657
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10574112/
Abstract

Osteoarthritis is a substantial burden for patients with the disease. The known medications for the disease target the mitigation of the disease's symptoms. So, drug development for the management of osteoarthritis represents an important challenge in the medical field. This work is based on the development of a new benzofuran-pyrazole-pyridine-based compound with potential anti-inflammatory and anti-osteoarthritis properties. Microanalytical and spectral data confirmed the chemical structure of compound . The biological assays indicated that compound produces multifunctional activity as an anti-osteoarthritic candidate via inhibition of pro-inflammatory mediators, including RANTES, CRP, COMP, CK, and LPO in OA rats. Histopathological and pharmacokinetic studies confirmed the safety profile of the latter molecule. Accordingly, compound is considered a promising anti-osteoarthritis agent and deserves deeper investigation in future trials.

摘要

骨关节炎是患者的沉重负担。该疾病的已知药物针对减轻疾病症状。因此,管理骨关节炎的药物开发代表了医学领域的重要挑战。这项工作基于具有潜在抗炎和抗骨关节炎特性的新型苯并呋喃-吡唑-吡啶基化合物的开发。微量分析和光谱数据证实了化合物的化学结构。生物学检测表明,化合物通过抑制促炎介质,包括 OA 大鼠中的 RANTES、CRP、COMP、CK 和 LPO,产生多功能活性,作为抗骨关节炎候选物。组织病理学和药代动力学研究证实了该分子的安全性概况。因此,化合物被认为是一种有前途的抗骨关节炎药物,值得在未来的试验中进行更深入的研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/512d/10574112/b4040440d994/molecules-28-06814-g006a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/512d/10574112/0082bcaf4828/molecules-28-06814-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/512d/10574112/68905e13becd/molecules-28-06814-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/512d/10574112/17b360096406/molecules-28-06814-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/512d/10574112/5c057f51a218/molecules-28-06814-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/512d/10574112/21458a497e00/molecules-28-06814-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/512d/10574112/cfb2b3bb9877/molecules-28-06814-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/512d/10574112/b4040440d994/molecules-28-06814-g006a.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/512d/10574112/0082bcaf4828/molecules-28-06814-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/512d/10574112/68905e13becd/molecules-28-06814-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/512d/10574112/17b360096406/molecules-28-06814-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/512d/10574112/5c057f51a218/molecules-28-06814-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/512d/10574112/21458a497e00/molecules-28-06814-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/512d/10574112/cfb2b3bb9877/molecules-28-06814-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/512d/10574112/b4040440d994/molecules-28-06814-g006a.jpg

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