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Source: Bioorganic and Medicinal Chemistry

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Total 18 results found since Jan 2013.

Growth factors and their peptide mimetics for treatment of traumatic brain injury
Bioorg Med Chem. 2023 Jun 10;90:117368. doi: 10.1016/j.bmc.2023.117368. Online ahead of print.ABSTRACTTraumatic brain injury (TBI) is a leading cause of disability in adults, caused by a physical insult damaging the brain. Growth factor-based therapies have the potential to reduce the effects of secondary injury and improve outcomes by providing neuroprotection against glutamate excitotoxicity, oxidative damage, hypoxia, and ischemia, as well as promoting neurite outgrowth and the formation of new blood vessels. Despite promising evidence in preclinical studies, few neurotrophic factors have been tested in clinical trials ...
Source: Bioorganic and Medicinal Chemistry - June 18, 2023 Category: Chemistry Authors: Emily Atkinson Rachael Dickman Source Type: research

Synthesis and bioactivity evaluation of a myelin-specific contrast agent for magnetic resonance imaging of myelination in central nervous system
Bioorg Med Chem. 2023 Mar 21;84:117257. doi: 10.1016/j.bmc.2023.117257. Online ahead of print.ABSTRACTDemyelination exists in many neurological diseases of nervous system, such as stroke. Currently, magnetic resonance imaging (MRI) has been the main tool for diagnosing and monitoring the myelin related diseases. However, the conventional MRI unable to distinguish demyelinating lesions from other inflammatory lesions. To address this problem, we have designed and prepared a myelin specific magnetic resonance contrast agent, Gd-DTDAS, which was based myelin specific moiety MeDASg and Gd-DTPAh. In this work, we verified the s...
Source: Bioorganic and Medicinal Chemistry - March 31, 2023 Category: Chemistry Authors: Bin Wei Na Weng Lei Fu Yuxuan Li Xu Wang Ruijuan Yin Tao Jiang Source Type: research

Design and synthesis of novel GluN2A NMDAR positive allosteric modulators via scaffold hopping strategy as anti-stroke therapeutic agents
This study reported a series of GluN1/2A positive allosteric modulators as neuroprotective agents, and provided a potential opportunity to discover new drugs for stroke treatment.PMID:36934527 | DOI:10.1016/j.bmc.2023.117236
Source: Bioorganic and Medicinal Chemistry - March 19, 2023 Category: Chemistry Authors: Xin Chen Hongyu Zhu Xuequan Liu Qihong Li Mingxin Dong Source Type: research

Synthesis and biological evaluation of hybrids from optically active ring-opened 3-N-butylphthalide derivatives and 4-fluro-edaravone as potential anti-acute ischemic stroke agents
Bioorg Med Chem. 2022 Jun 20;69:116891. doi: 10.1016/j.bmc.2022.116891. Online ahead of print.ABSTRACTThe treatment of acute ischemic stroke (AIS) remains a tough challenge in clinic. Here, we report the anti-AIS activity of R- and S-FMPB generated from hybridization of ring-opened R- and S-3-N-butylphthalide (R- and S-NBP) derivatives (R- and S-APB) with 4-fluro-edaravone (4-F-Eda), respectively. S-FMPB (10 mg/kg, iv) significantly improved the neurological score and alleviated cerebral infarction and edema of rats suffered from transient middle cerebral artery occlusion (tMCAO), superior to RS- and R-FMPB, as well as bet...
Source: Bioorganic and Medicinal Chemistry - June 28, 2022 Category: Chemistry Authors: Jian Jia Jianbing Wu Duorui Ji Weijie Jiao Xiaoli Wang Zhangjian Huang Yihua Zhang Source Type: research

Targeting NLRP3 signaling by a novel-designed sulfonylurea compound for inhibition of microglial inflammation
Bioorg Med Chem. 2022 Jan 31;58:116645. doi: 10.1016/j.bmc.2022.116645. Online ahead of print.ABSTRACTThe nucleotide-binding oligomerization domain (NOD)-like receptor protein 3 (NLRP3) inflammasome plays an important role in microglia-mediated inflammation. Dysregulation of NLRP3 signaling results in microglial activation and triggers inflammatory responses contributing to the development of neurological disorders including ischemic stroke, schizophrenia, Alzheimer's disease (AD), Parkinson's disease (PD), and amyotrophic lateral sclerosis (ALS). Inhibition of the NLRP3-linked inflammatory pathways reduces microglia-induc...
Source: Bioorganic and Medicinal Chemistry - February 12, 2022 Category: Chemistry Authors: Changwen Zhang Ayyiliath M Sajith Xiaotian Xu Jianxiong Jiang J Phillip Bowen Amol Kulkarni Jiukuan Hao Source Type: research

AMPK inhibitor BML-275 induces neuroprotection through decreasing cyt c and AIF expression after transient brain ischemia
This study supports the hypothesis that anti-apoptosis is one of potential neuroprotective strategies for the treatment of stroke.PMID:34837819 | DOI:10.1016/j.bmc.2021.116522
Source: Bioorganic and Medicinal Chemistry - November 27, 2021 Category: Chemistry Authors: Yue Hu Yao-Dong Dong Yan-Chao Wu Qiu-Xu Wang Xiang Nan Da-Li Wang Source Type: research

Discovery of neuroprotective agents that inhibit human prolyl hydroxylase PHD2
Bioorg Med Chem. 2021 Mar 24;38:116115. doi: 10.1016/j.bmc.2021.116115. Online ahead of print.ABSTRACTProlyl hydroxylase (PHD) enzymes play a critical role in the cellular responses to hypoxia through their regulation of the hypoxia inducible factor α (HIF-α) transcription factors. PHD inhibitors show promise for the treatment of diseases including anaemia, cardiovascular disease and stroke. In this work, a pharmacophore-based virtual high throughput screen was used to identify novel potential inhibitors of human PHD2. Two moderately potent new inhibitors were discovered, with IC50 values of 4 μM and 23 μM respectively...
Source: Bioorganic and Medicinal Chemistry - April 16, 2021 Category: Chemistry Authors: Nicole L Richardson Laura J O'Malley Daniel Weissberger Anthony Tumber Christopher J Schofield Renate Griffith Nicole M Jones Luke Hunter Source Type: research

Fibroblast growth factor receptor modulators employing diamines with reduced phospholipidosis-inducing potential.
Abstract SUN13837 (1), a fibroblast growth factor receptor modulator, has been an attractive candidate for treating neurodegenerative diseases. However, one of its metabolites, N-benzyl-4-(methylamino)piperidine (BMP), turned out to possess phospholipidosis-inducing potential (PLIP) in vitro. To obtain SUN13837 analogs with reduced phospholipidosis risk, we replaced BMP with other diamines possessing low PLIP. Our effort led to the discovery of compound 6 with increased efficacy. Further structural modifications to reduce hydrogen bond donors afforded 17 with improved brain exposure. Oral administration of 17 at 1...
Source: Bioorganic and Medicinal Chemistry - July 5, 2020 Category: Chemistry Authors: Sakai H, Inoue H, Murata K, Toba T, Shimmyo Y, Narii N, Ueno SY, Igawa Y, Takemoto N Tags: Bioorg Med Chem Source Type: research

Chemical reactivity and uses of 1-phenyl-3-methyl-5-pyrazolone (PMP), also known as edaravone.
Abstract 1-Phenyl-3-methyl-5-pyrazolone is a reagent, known as PMP, used to derivatize monosaccharides for the study of polysaccharides composition and structure, and for the dosage of carbohydrates in complex media. The same molecule is also known as edaravone, a drug approved for the treatment of stroke and amyotrophic lateral sclerosis. It is also a reactive molecule susceptible to form stable adducts with aromatic aldehydes, such as formylpterin and vanillin. In addition, the molecule serves as a scaffold to design of edaravone analogs and drug conjugates, with various pharmacological properties (antioxidant, ...
Source: Bioorganic and Medicinal Chemistry - March 24, 2020 Category: Chemistry Authors: Bailly C, Hecquet PE, Kouach M, Thuru X, Goossens JF Tags: Bioorg Med Chem Source Type: research