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Source: European Journal of Medicinal Chemistry
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Total 35 results found since Jan 2013.
Synthesis of 1,3,5-triphenyl-1,2,4-triazole derivatives and their neuroprotection by anti-oxidative stress and anti-inflammation and protecting BBB
Eur J Med Chem. 2023 Aug 21;260:115742. doi: 10.1016/j.ejmech.2023.115742. Online ahead of print.ABSTRACTAcute ischemic stroke (AIS) is a serious cardiovascular and cerebrovascular disease; Oxidative stress and neuroinflammation are important factors which destroy blood-brain barrier (BBB) in AIS. In the study, a series of 1,3,5-triphenyl-1,2,4-triazole derivatives were designed and synthesized; the optimal compound 9 was obtained by screening their anti-oxidant and anti-inflammatory effects; the neuroprotection effect of compound 9 was evaluated with a rat middle cerebral artery occlusion (MCAO) model. Subsequently, the m...
Source: European Journal of Medicinal Chemistry - August 31, 2023 Category: Chemistry Authors: Yang Wang Ruiqi Su Jianwen Chen Xuan Liu Jingning Luo Yaoqiang Lao Ping Huang Jinguo Shi Caibao Jiang Liping Liao Jingxia Zhang Source Type: research
Small molecule inhibitors of NLRP3 inflammasome and GSK-3 β in the management of traumatic brain injury: A review
Eur J Med Chem. 2023 Aug 9;259:115718. doi: 10.1016/j.ejmech.2023.115718. Online ahead of print.ABSTRACTTraumatic brain injury (TBI) is a debilitating mental condition which causes physical disability and morbidity worldwide. TBI may damage the brain by direct injury that subsequently triggers a series of neuroinflammatory events. The activation of NLRP3 inflammasome and dysregulated host immune system has been documented in various neurological disorders such as TBI, ischemic stroke and multiple sclerosis. The activation of NLRP3 post-TBI increases the production of pro-inflammatory cytokines and caspase-1, which are majo...
Source: European Journal of Medicinal Chemistry - August 13, 2023 Category: Chemistry Authors: Mahammad Ghouse Shaik Swanand Vinayak Joshi Ravikumar Akunuri Preeti Rana Ziaur Rahman Anusha Polomoni Venkata Madhavi Yaddanapudi Manoj P Dandekar Nanduri Srinivas Source Type: research
Perspectives and new aspects of histone deacetylase inhibitors in the therapy of CNS diseases
Eur J Med Chem. 2023 Jun 29;258:115613. doi: 10.1016/j.ejmech.2023.115613. Online ahead of print.ABSTRACTMany populations worldwide are suffering from central nervous system (CNS) diseases such as brain tumors, neurodegenerative diseases (Alzheimer's disease, Parkinson's disease and Huntington's disease) and stroke. There is a shortage of effective drugs for most CNS diseases. As one of the regulatory mechanisms of epigenetics, the particular role and therapeutic benefits of histone deacetylases (HDACs) in the CNS have been extensively studied. In recent years, HDACs have attracted increasing attention as potential drug ta...
Source: European Journal of Medicinal Chemistry - July 3, 2023 Category: Chemistry Authors: Bo Han Mengfei Wang Jiayi Li Qiushi Chen Niubing Sun Xuezhi Yang Qingwei Zhang Source Type: research
Inhibition of the pyroptosis-associated inflammasome pathway: The important potential mechanism of ginsenosides in ameliorating diabetes and its complications
Eur J Med Chem. 2023 Apr 5;253:115336. doi: 10.1016/j.ejmech.2023.115336. Online ahead of print.ABSTRACTDiabetes mellitus (DM) and its complications have become an important global public health issue, affecting human health and negatively impacting life and lifespan. Pyroptosis is a recently discovered form of pro-inflammatory programmed cell death (PCD). To date, pyroptosis-associated inflammasome pathways have been identified primarily in the canonical and non-canonical inflammasome pathway, apoptotic caspase-mediated pathway, granzyme-mediated pathway, and streptococcal pyrogenic exotoxin B (SpeB)-mediated pathway. The...
Source: European Journal of Medicinal Chemistry - April 9, 2023 Category: Chemistry Authors: Pan Liu Zhengdong Zhang Yichen Cai Yunjiao Yang Jun Yuan Qiu Chen Source Type: research
Development of sertraline analogues as potential anti-ischemic stroke agents
Eur J Med Chem. 2023 Mar 15;252:115273. doi: 10.1016/j.ejmech.2023.115273. Online ahead of print.ABSTRACTIschemic stroke (IS) is harmful to human health and social development, and there is no medicine available at present. To find the hit compound for treating ischemic stroke, we screened 28 FDA approved nervous system drugs by using an in vitro OGD-induced stroke model. Notably, our in vitro and in vivo studies demonstrated that low-dose sertraline had good neuroprotective activities, while high-dose sertraline showed significant toxicity. Interestingly, the same high-dose sertraline in the control group did not exhibit ...
Source: European Journal of Medicinal Chemistry - March 22, 2023 Category: Chemistry Authors: Xin Chen Hong-Yuan Liu Sheng-Li Niu Ting Zhou Wen Yuan Peng-Fei Zheng Qiong Chen Su-Lan Luo Jing Gu Dong-Ting Zhangsun Qin Ouyang Source Type: research
Discovery of phenylcarbamoyl xanthone derivatives as potent neuroprotective agents for treating ischemic stroke
Eur J Med Chem. 2023 Mar 7;251:115251. doi: 10.1016/j.ejmech.2023.115251. Online ahead of print.ABSTRACTCompounds of natural sources are widespread discovered in the treatment of ischemic stroke. Alpha-mangostin, a natural prenylated xanthone, has been found to display a therapeutic potential to treat ischemic stroke. However, the direct application of α-mangostin is limited due to its cytotoxicity and relatively low efficacy. Herein, structural modification of α-mangostin was necessary to improve its drug-ability. Currently, 34 α-mangostin phenylcarbamoyl derivatives were synthesized and evaluated for their neuroprotec...
Source: European Journal of Medicinal Chemistry - March 15, 2023 Category: Chemistry Authors: Yi-Li Chen Yu-Chen Chen Lin-An Xiong Qu-Yang Huang Ting-Ting Gong Yan Chen Lie-Feng Ma Luo Fang Zha-Jun Zhan Source Type: research
Design and synthesis of novel indole and indazole-piperazine pyrimidine derivatives with anti-inflammatory and neuroprotective activities for ischemic stroke treatment
In conclusion, 5j has the potential for the treatment of stroke as an anti-inflammatory and neuroprotective agent.PMID:35931005 | DOI:10.1016/j.ejmech.2022.114597
Source: European Journal of Medicinal Chemistry - August 5, 2022 Category: Chemistry Authors: Hongwei Wang Enjing Cui Jiaming Li Xiaodong Ma Xueyang Jiang Shuaishuai Du Shihu Qian Le Du Source Type: research
Synthesis and biological evaluation of 1,2,4-triazole derivatives as potential Nrf2 activators for the treatment of cerebral ischemic injury
Eur J Med Chem. 2022 Mar 28;236:114315. doi: 10.1016/j.ejmech.2022.114315. Online ahead of print.ABSTRACTAcute ischemic stroke is a leading cause of disability and death. The development of neuroprotectants is an emerging strategy for the treatment of ischemic stroke. In this work, we designed and synthesized a series of 1,3,5-triaryl substituent triazole derivatives by introducing a phenolic group and phenyl ring to 3,5-diaryl substituents oxadiazole. Structure-activity relationship (SAR) analysis showed that compounds with alkyl groups or with substituents at the 3-position possessed better protective effects. Among the ...
Source: European Journal of Medicinal Chemistry - April 7, 2022 Category: Chemistry Authors: Yaoqiang Lao Yang Wang Jianwen Chen Ping Huang Ruiqi Su Jinguo Shi Caibao Jiang Jingxia Zhang Source Type: research
