阿巴芬净(Abafungin) - 药物靶点：SMT1_在研适应症：真菌病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Abasol

+ [4]

靶点

SMT1

作用机制

SMT1抑制剂(24-甾醇C-甲基转移酶抑制剂)

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

Ludwig-Maximilians-Universität München

Bayer AGYork Pharma Gmbh

非在研机构-

最高研发阶段药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C21H22N4OS

InChIKeyTYBHXIFFPVFXQW-UHFFFAOYSA-N

CAS号129639-79-8

关联

3

项与阿巴芬净相关的临床试验

EUCTR2007-002112-26-HU / Unknown statusN/A

Open, single-arm phase-III study to investigate the percutaneous absorption of abafungin after topical dermal application of Abafungin cream 1.0 % (YORK Pharma GmbH) in 20 patients with tinea pedis interdigitalis

开始日期2007-05-21

申办/合作机构

York Pharma Gmbh

EUCTR2006-001263-32-DE / Not yet recruitingN/A

Phase III study to evaluate the anti-mycotic efficacy of a topical Abafungin formulation in patients with tinea pedis - N.A.

开始日期2006-06-29

申办/合作机构

York Pharma Gmbh

EUCTR2005-002842-20-DE / Not yet recruitingN/A

Phase II dose ranging study to evaluate the anti-mycotic efficacy of topical Abafungin formulations in patients with tinea pedis. - N.A.

开始日期2005-09-29

申办/合作机构

York Pharma Gmbh

100 项与阿巴芬净相关的临床结果

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100 项与阿巴芬净相关的转化医学

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100 项与阿巴芬净相关的专利（医药）

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8

项与阿巴芬净相关的文献（医药）

2024-06-05·Journal of Agricultural and Food Chemistry

Walnut-Derived Peptides Ameliorate Scopolamine-Induced Memory Impairments in a Mouse Model via Activation of Peroxisome Proliferator-Activated Receptor γ-Mediated Excitotoxicity

Article

作者: Li, Yanru ; Dang, Qiao ; Liu, Chunlei ; Wu, Dan ; Min, Weihong ; Zhao, Fanrui ; Fang, Li ; Shen, Yue

We investigated the protective effect of walnut peptides and YVPFPLP (YP-7) on scopolamine-induced memory impairment in mice and β-amyloid (Aβ)-induced excitotoxic injury in primary hippocampal neurons, respectively. Additionally, the protective mechanism of YP-7 on neuronal excitotoxicity was explored. Mouse behavioral and hippocampal slice morphology experiments indicate that YP-7 improves the learning and memory abilities of cognitively impaired mice and protects synaptic integrity. Immunofluorescence, western blotting, and electrophysiological experiments on primary hippocampal neurons indicate that YP-7 inhibits neuronal damage caused by excessive excitation of neurons induced by Aβ. HT-22 cell treatment with peroxisome proliferator-activated receptor γ (PPARγ) activators and inhibitors showed that YP-7 activates PPARγ expression and maintains normal neuronal function by forming stable complexes with PPARγ to inhibit the extracellular regulated protein kinase pathway. Therefore, YP-7 can ameliorate glutamate-induced excitotoxicity and maintain neuronal signaling. This provides a theoretical basis for active peptides to ameliorate excitotoxicity and the development of functional foods.

2023-01-01·Current topics in medicinal chemistry

1,3-thiazole Derivatives: A Scaffold with Considerable Potential in the Treatment of Neurodegenerative Diseases.

Review

作者: Gupta, Jatin ; Chaudhary, Jasmine ; Sharma, Vishal ; Jain, Akash ; Kaushik, Aditi ; Dhingra, Ashwani ; Chopra, Bhawna

1,3-thiazoles, which contain nitrogen and a sulfur atom is an unsaturated five-membered heterocyclic ring, have achieved a unique significant place in drug design and development because of their versatile structure and a variety of pharmacological activities, viz. anticancer, antiviral, antimicrobial, anticonvulsant, antioxidant, antidiabetic, etc. They have inspired researchers to design novel thiazole with different biological activities. The presence of the thiazole moiety has resulted in a large number of clinically useful drugs with a wide range of activities, such as Ritonavir (antiviral), Sulfathiazole (antimicrobial antibiotic), Abafungin, Ravuconazole (antifungal), Meloxicam (NSAID), etc., that further verify this statement. The prevalence of neurodegenerative diseases like Alzheimer's, Parkinson's, and Huntington's is increasing at a rapid pace but existing treatments mainly provide symptomatic relief and are associated with undesired effects. Consequently, designing novel compounds with more effectiveness and reduced toxicity are required. 1,3-thiazole derivatives have emerged as excellent candidate in this regard and have an important role for the treatment of neurodegenerative diseases. In the current review, we have gathered all the appropriate literature which demonstrate the remarkable role of 1,3-thiazole and its derivatives in these diseases that may help design new compounds with more desired characteristics. The literature was assessed through worldwide scientific databases like GOOGLE, SCOPUS, and PUBMED using different keywords, and only relevant information published in English was evaluated.

2018-12-01·Chemistry Central Journal

Stereoselective synthesis, X-ray analysis, computational studies and biological evaluation of new thiazole derivatives as potential anticancer agents

Article

作者: Soliman, Saied M ; Ghabbour, Hazem A ; Al-Showiman, Salim S ; Kheder, Nabila A ; Frey, Wolfgang ; Mabkhot, Yahia N ; Alharbi, Mohammed M

BACKGROUNDThe synthesis of new thiazole derivatives is very important because of their diverse biological activities. Also , many drugs containing thiazole ring in their skeletons are available in the market such as Abafungin, Acotiamide, Alagebrium, Amiphenazole, Brecanavir, Carumonam, Cefepime, and Cefmatilen.RESULTSEthyl cyanoacetate reacted with phenylisothiocyanate, chloroacetone, in two different basic mediums to afford the thiazole derivative 6, which reacted with dimethylformamide- dimethyl acetal in the presence of DMF to afford the unexpected thiazole derivative 11. The structures of the thiazoles 6 and 11 were optimized using B3LYP/6-31G(d,p) method. The experimentally and theoretically geometric parameters agreed very well. Also, the natural charges at the different atomic sites were predicted. HOMO and LUMO demands were discussed. The anticancer activity of the prepared compounds was evaluated and showed moderate activity.CONCLUSIONSSynthesis of novel thiazole derivatives was done. The structure was established using X-ray and spectral analysis. Optimized molecular structures at the B3LYP/6-31G(d,p) level were investigated. Thiazole derivative 11 has more electropositive S-atom than thiazole 6. The HOMO-LUMO energy gap is lower in the former compared to the latter. The synthesized compounds showed moderate anticancer activity.

100 项与阿巴芬净相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	阿巴芬净	-	DB06395

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
真菌病	药物发现	-	Ludwig-Maximilians-Universität München	2008-06-30
真菌病	药物发现	-	York Pharma Gmbh	2008-06-30
真菌病	药物发现	德国	Bayer AG	2008-06-30
足癣	药物发现	德国	York Pharma Gmbh	2006-11-18