33282-17-6Relevant 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-
COMPOUNDS AND USES THEREOF
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Paragraph 0696; 1160, (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.
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).
Synthesis and anticancer activity of heteroaromatic linked 4β-amido podophyllotoxins as apoptotic inducing agents
Kamal, Ahmed,Tamboli, Jaki R.,Vishnuvardhan,Adil,Nayak, V. Lakshma,Ramakrishna
, p. 273 - 280 (2013/02/25)
A series of different heteroaromatic linked 4β-amidopodophyllotoxin conjugates (16a-i, 17a-i and 18a-d) were synthesized and evaluated for anticancer activity against five human cancer cell lines. Among the series, one of the compound 17g showed significant antiproliferative activity in A549 (lung cancer) cell line. Flow cytometric analysis showed that 17g arrested the cell cycle in the G2/M phase leading to caspase-3 dependent apoptotic cell death. Further, Hoechst 33258 staining and DNA fragmentation assay also suggests that 17g induces cell death by apoptosis.
