338982-35-7Relevant academic research and scientific papers
Novel N-benzylpiperidine derivatives of 5-arylisoxazole-3-carboxamides as anti-Alzheimer's agents
Saeedi, Mina,Felegari, Peyman,Iraji, Aida,Hariri, Roshanak,Rastegari, Arezoo,Mirfazli, S. Sara,Edraki, Najmeh,Firuzi, Omidreza,Mahdavi, Mohammad,Akbarzadeh, Tahmineh
, (2020/11/30)
The complex pathophysiology of Alzheimer's disease (AD) has prompted researchers to develop multitarget-directed molecules to find an effective therapy against the disease. In this context, a novel series of N-(1-benzylpiperidin-4-yl)-5-arylisoxazole-3-ca
Design and synthesis of novel 5-arylisoxazole-1,3,4-thiadiazole hybrids as α-glucosidase inhibitors
Akbarzadeh, Tahmineh,Eslami, Azadeh,Faramarzi, Mohammad Ali,Mahdavi, Mohammad,Mirfazli, Seyedeh Sara,Saeedi, Mina,Zardkanlou, Mahsa
, p. 436 - 444 (2021/10/04)
Background: α-Glucosidase inhibitors have occupied a significant position in the treatment of type 2 diabetes. In this respect, the development of novel and efficient non-sugar-based inhibitors is in high demand. Objective: Design and synthesis of new 5-arylisoxazole-1,3,4-thiadiazole hybrids possessing α-glucosidase inhibitory activity were developed. Methods: Different derivatives were synthesized by the reaction of various 5-arylisoxazole-3-carboxylic acids and ethyl 2-((5-amino-1,3,4-thiadiazol-2-yl)thio)acetate. Finally, they were evalu-ated for their α-glucosidase inhibitory activity. Results: It was found that ethyl 2-((5-(5-(2-chlorophenyl)isoxazole-3-carboxamido)-1,3,4-thiadiazol-2-yl)thio)acetate (5j) was the most potent compound (IC50 = 180.1 μM) compared with acarbose as the reference drug (IC50 = 750.0 μM). Also, the kinetic study of 5j revealed a competitive inhibition and docking study results indicated desired interactions of that compound with amino acid residues located close to the active site of α-glucosidase. Conclusion: Good α-glucosidase inhibitory activity obtained by the title compounds introduced them as an efficient scaffold, which merits to be considered in anti-diabetic drug discovery developments.
Design and Synthesis of Novel Arylisoxazole-Chromenone Carboxamides: Investigation of Biological Activities Associated with Alzheimer's Disease
Akbarzadeh, Tahmineh,Edraki, Najmeh,Firuzi, Omidreza,Hariri, Roshanak,Mahdavi, Mohammad,Mirfazli, Seyedeh Sara,Rastegari, Arezoo,Saeedi, Mina
, (2020/04/29)
A novel series of hybrid arylisoxazole-chromenone carboxamides were designed, synthesized, and evaluated for their cholinesterase (ChE) inhibitory activity based on the modified Ellman's method. Among synthesized compounds, 5-(3-nitrophenyl)-N-{4-[(2-oxo-
Rational modification, synthesis and biological evaluation of 3,4-dihydroquinoxalin-2(1H)-one derivatives as potent and selective c-Jun N-terminal kinase 3 (JNK3) inhibitors
Dou, Xiaodong,Huang, Huixia,Jiang, Lan,Jiao, Ning,Jin, Hongwei,Liu, Zhenming,Zhang, Liangren,Zhang, Lihe,Zhu, Guiwang
, (2020/07/03)
The c-Jun N-terminal kinase 3 (JNK3) plays key roles in a wide range of diseases, including neurodegeneration diseases, inflammation diseases, cancers, cardiovascular diseases, and metabolic disorders. Previously, we have identified a lead compound, (Z)-3
Green and efficient synthesis of new pyrido[2,3-d]pyrimidine derivatives using Pd/SBA-15 as a nanocatalyst
Bardajee, Ghasem Rezanejade,Delbari, Akram Sadat,Ghaedi, Aseyeh,Hekmat, Shohreh
, (2020/09/07)
N-Fused heterocycles have received significant attention over the years as valuable compounds due to their biological and pharmaceutical activities. Heterogeneous catalysts such as periodic mesoporous materials have played an important role in the synthes
Fragment-based lead generation of 5-phenyl-1H-pyrazole-3-carboxamide derivatives as leads for potent factor xia inhibitors
Wei, Qunchao,Zheng, Zhichao,Zhang, Shijun,Zheng, Xuemin,Meng, Fancui,Yuan, Jing,Xu, Yongnan,Huang, Changjiang
, (2018/09/26)
FXIa is suggested as a major target for anticoagulant drug discovery because of reduced risk of bleeding. In this paper, we defined 5-phenyl-1H-pyrazole-3-carboxylic acid derivatives as privileged fragments for FXIa inhibitors' lead discovery. After repla
Simple and efficient syntheses of novel benzo[4,5]imidazo[1,2-a]pyridine derivatives
Goli-Garmroodi, Fereshteh,Omidi, Marzieh,Saeedi, Mina,Sarrafzadeh, Farhad,Rafinejad, Ali,Mahdavi, Mohammad,Bardajee, Ghasem Rezanejade,Akbarzadeh, Tahmineh,Firoozpour, Loghman,Shafiee, Abbas,Foroumadi, Alireza
, p. 743 - 746 (2015/01/30)
A novel series of benzo[4,5]imidazo[1,2-a]pyridine derivatives is synthesized through the reaction of 2-(1H-benzo[d]imidazol-2-yl)acetonitrile and different ethyl 2,4-dioxo-4-arylbutanoate derivatives in the presence of piperidine in refluxing EtOH. All the products are easily prepared within 25-45 min in good to excellent yields.
Facile, novel and efficient synthesis of new pyrazolo[3,4-b]pyridine products from condensation of pyrazole-5-amine derivatives and activated carbonyl groups
Ghaedi,Bardajee,Mirshokrayi,Mahdavi,Shafiee,Akbarzadeh
, p. 89652 - 89658 (2015/11/10)
An efficient synthesis of novel ethyl-1,3,4-triphenyl-1H-pyrazolo[3,4-b]pyridine-6-carboxylate products has been achieved via condensation of pyrazole-5-amine derivatives and activated carbonyl groups, in refluxing acetic acid. This process has been found to be useful in the preparation of new N-fused heterocycle products in good to excellent yields.
Structure-activity studies of a novel series of isoxazole-3-carboxamide derivatives as TRPV1 antagonists
Palin, Ronald,Abernethy, Lynn,Ansari, Nasrin,Cameron, Kenneth,Clarkson, Tom,Dempster, Maureen,Dunn, David,Easson, Anna-Marie,Edwards, Darren,MacLean, John,Everett, Katy,Feilden, Helen,Ho, Koc-Kan,Kultgen, Steve,Littlewood, Peter,McArthur, Duncan,McGregor, Deborah,McLuskey, Hazel,Neagu, Irina,Neale, Stuart,Nisbet, Lesley-Anne,Ohlmeyer, Michael,Pham, Quynhchi,Ratcliffe, Paul,Rong, Yajing,Roughton, Andrew,Sammons, Melanie,Swanson, Robert,Tracey, Heather,Walker, Glenn
scheme or table, p. 892 - 898 (2011/03/21)
Optimisation of a screening hit incorporating both TRPV1 activity and solubility was conducted. Substitution of the isoxazole-3-carboxamide with the bespoke 1S, 3R-3-aminocyclohexanol motif afforded the requisite balance of potency and solubility. Compounds 32 and 40 were found to have antihyperalgesic effects in the rat CFA Hg assay and induce a mechanism based hyperthermia.
PYRAZOLE CARBOXAMIDES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE-1
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Page/Page column 30, (2010/02/10)
Pyrazole carboxamides of structural formula (I) are selective inhibitors of the 11beta-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin r
