- Novel N-benzylpiperidine derivatives of 5-arylisoxazole-3-carboxamides as anti-Alzheimer's agents
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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
- Saeedi, Mina,Felegari, Peyman,Iraji, Aida,Hariri, Roshanak,Rastegari, Arezoo,Mirfazli, S. Sara,Edraki, Najmeh,Firuzi, Omidreza,Mahdavi, Mohammad,Akbarzadeh, Tahmineh
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- Design and Synthesis of Selective Acetylcholinesterase Inhibitors: Arylisoxazole-Phenylpiperazine Derivatives
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In this work, a novel series of arylisoxazole-phenylpiperazines were designed, synthesized, and evaluated toward acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Our results revealed that [5-(2-chlorophenyl)-1,2-oxazol-3-yl](4-phenylpiperazin
- Saeedi, Mina,Mohtadi-Haghighi, Dorrin,Mirfazli, Seyedeh Sara,Mahdavi, Mohammad,Hariri, Roshanak,Lotfian, Hania,Edraki, Najmeh,Iraji, Aida,Firuzi, Omidreza,Akbarzadeh, Tahmineh
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- Design, synthesis and structure-based optimization of novel isoxazole-containing benzamide derivatives as FtsZ modulators
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Antibiotic resistance among clinically significant bacterial pathogens is becoming a prevalent threat to public health, and new antibacterial agents with novel mechanisms of action hence are in an urgent need. Utilizing computational docking method and structure-based optimization strategy, we rationally designed and synthesized two series of isoxazol-3-yl- and isoxazol-5-yl-containing benzamide derivatives that targeted the bacterial cell division protein FtsZ. Evaluation of their activity against a panel of Gram-positive and -negative pathogens revealed that compounds B14 and B16 that possessed the isoxazol-5-yl group showed strong antibacterial activity against various testing strains, including methicillin-resistant Staphylococcus aureus and penicillin-resistant S. aureus. Further molecular biological studies and docking analyses proved that the compound functioned as an effective inhibitor to alter the dynamics of FtsZ self-polymerization via a stimulatory mechanism, which finally terminated the cell division and caused cell death. Taken together, these results could suggest a promising chemotype for development of new FtsZ-targeting bactericidal agent.
- Bi, Fangchao,Song, Di,Zhang, Nan,Liu, Zhiyang,Gu, Xinjie,Hu, Chaoyu,Cai, Xiaokang,Venter, Henrietta,Ma, Shutao
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- Novel indole-isoxazole hybrids: Synthesis and in vitro anti-cholinesterase activity
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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
- Vafadarnejad, Fahimeh,Saeedi, Mina,Mahdavi, Mohammad,Rafinejad, Ali,Karimpour-Razkenari, Elahe,Sameem, Bilqees,Khanavi, Mahnaz,Akbarzadeh, Tahmineh
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p. 712 - 717
(2017/07/15)
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- 2-Amino-3-cyano-4-(5-arylisoxazol-3-yl)-4H-chromenes: Synthesis and in vitro cytotoxic activity
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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
- Akbarzadeh, Tahmineh,Rafinejad, Ali,Mollaghasem, Javad Malekian,Safavi, Maliheh,Fallah-Tafti, Asal,Pordeli, Mahboobeh,Ardestani, Sussan Kabudanian,Shafiee, Abbas,Foroumadi, Alireza
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experimental part
p. 386 - 392
(2012/07/27)
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