371157-17-4Relevant articles and documents
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.
Development of a continuous flow photoisomerization reaction converting isoxazoles into diverse oxazole products
Bracken, Cormac,Baumann, Marcus
, p. 2607 - 2617 (2020/03/11)
A continuous flow process is presented, which directly converts isoxazoles into their oxazole counterparts via a photochemical transposition reaction. This results in the first reported exploitation of this transformation to establish its scope and synthe
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-
COMPOUNDS AND USES THEREOF
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Paragraph 0694; 1158, (2019/11/11)
The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
Novel hybrid molecules of isoxazole chalcone derivatives: Synthesis and study of In Vitro cytotoxic activities
Thiriveedhi, Arunkumar,Nadh, Ratnakaram Venkata,Srinivasu, Navuluri,Kaushal, Kishore
, p. 576 - 582 (2018/06/06)
Background: Now-a-days, the model of “hybrid drugs” has acquired recognition in medicine due to their significant role in the treatment of different health problems. Methods: We have synthesized new series of isoxazole-chalcone conjugates (14a-m) by the C
1,2,3-Triazole-isoxazole based acetylcholinesterase inhibitors: Synthesis, biological evaluation and docking study
Najafi, Zahra,Mahdavi, Mohammad,Saeedi, Mina,Sabourian, Reyhaneh,Khanavi, Mahnaz,Safavi, Maliheh,Tehrani, Maliheh Barazandeh,Shafiee, Abbas,Foroumadi, Alireza,Akbarzadeh, Tahmineh
, p. 58 - 65 (2017/05/08)
In this work, a series of derivatives containing 1,2,3-triazole and isoxazole were synthesized. All of them were evaluated as novel dual AChE inhibitors. Most of synthesized compounds showed moderate to good inhibitory potency toward AChE. Among them, N-(
Novel indole-isoxazole hybrids: Synthesis and in vitro anti-cholinesterase activity
Vafadarnejad, Fahimeh,Saeedi, Mina,Mahdavi, Mohammad,Rafinejad, Ali,Karimpour-Razkenari, Elahe,Sameem, Bilqees,Khanavi, Mahnaz,Akbarzadeh, Tahmineh
, p. 712 - 717 (2017/07/15)
Background: This work reports synthesis and in vitro cholinesterase inhibitory activity of novel indole-isoxazole hybrids. Method: The synthetic procedure was started from different ethyl 5-Arylisoxazole-3-carboxylate derivatives. Hydrolysis and reaction
Synthesis and in Vitro Cytotoxic Activity of Novel Triazole-Isoxazole Derivatives
Najafi, Zahra,Mahdavi, Mohammad,Safavi, Maliheh,Saeedi, Mina,Alinezhad, Heshmatollah,Pordeli, Mahboobeh,Kabudanian Ardestani, Sussan,Shafiee, Abbas,Foroumadi, Alireza,Akbarzadeh, Tahmineh
, p. 1743 - 1747 (2015/11/09)
New derivatives of triazole-isoxazole were synthesized through a four-step reaction starting from various ethyl 4-aryl-2,4-dioxobutanoate derivatives. Finally, all compounds were examined by MTT assays for cytotoxic activity in two human breast cancer cell lines (MCF-7 and T-47D).
2-Amino-3-cyano-4-(5-arylisoxazol-3-yl)-4H-chromenes: Synthesis and in vitro cytotoxic activity
Akbarzadeh, Tahmineh,Rafinejad, Ali,Mollaghasem, Javad Malekian,Safavi, Maliheh,Fallah-Tafti, Asal,Pordeli, Mahboobeh,Ardestani, Sussan Kabudanian,Shafiee, Abbas,Foroumadi, Alireza
experimental part, p. 386 - 392 (2012/07/27)
A new series of 4-aryl-4H-chromenes bearing a 5-arylisoxazol-3-yl moiety at the C-4 position were prepared as potential anticancer agents. The in vitro cytotoxic activity of the synthesized compounds was investigated against a panel of tumor cell lines in