159670-70-9Relevant 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
Synthesis of isoxazoles via cyclization of β-fluoro enones with sodium azide
Li, Liangkui,Huang, Shiqing,Mao, Kuantao,Lv, Leiyang,Li, Zhiping
supporting information, (2021/04/22)
A practical method for the synthesis of 3,5-disubstituted isoxazoles via cyclization of β-fluoro enones with sodium azide was disclosed. Density functional theory (DFT) calculation indicated that both (1) the azirine formation followed by intramolecular rearrangement and (2) direct enolate O-attack via 5-exo-trig cyclization of vinyl azide were possible for the isoxazole formation.
Discovery of Membrane-Bound Pyrophosphatase Inhibitors Derived from an Isoxazole Fragment
Johansson, Niklas G.,Turku, Ainoleena,Vidilaseris, Keni,Dreano, Lo?c,Khattab, Ayman,Ayuso Pérez, Daniel,Wilkinson, Aaron,Zhang, Yuezhou,Tamminen, Matti,Grazhdankin, Evgeni,Kiriazis, Alexandros,Fishwick, Colin W. G.,Meri, Seppo,Yli-Kauhaluoma, Jari,Goldman, Adrian,Boije Af Genn?s, Gustav,Xhaard, Henri
, p. 605 - 610 (2020/03/10)
Membrane-bound pyrophosphatases (mPPases) regulate energy homeostasis in pathogenic protozoan parasites and lack human homologues, which makes them promising targets in e.g. malaria. Yet only few nonphosphorus inhibitors have been reported so far. Here, w
Oxidize Amines to Nitrile Oxides: One Type of Amine Oxidation and Its Application to Directly Construct Isoxazoles and Isoxazolines
Zhang, Xiao-Wei,He, Xiao-Lin,Yan, Nan,Zheng, Hong-Xing,Hu, Xiang-Guo
, p. 15726 - 15735 (2020/11/30)
A facile oxidative heterocyclization of commercially available amines and tert-butyl nitrite with alkynes or alkenes leading to isoxazoles or isoxazolines is described. The unprecedented strategy of the oxidation of an amine directly to a nitrile oxide was used in this cyclization process. This reaction is highly efficient, regiospecific, operationally simple, mild, and tolerant of a variety of functional groups. Control experiments support a nitrile oxide intermediate mechanism for this novel class of oxidative cyclization reactions. Moreover, synthetic applications toward bioactive molecular skeletons and the late-stage modification of drugs were realized.
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-
Design and Synthesis of Selective Acetylcholinesterase Inhibitors: Arylisoxazole-Phenylpiperazine Derivatives
Saeedi, Mina,Mohtadi-Haghighi, Dorrin,Mirfazli, Seyedeh Sara,Mahdavi, Mohammad,Hariri, Roshanak,Lotfian, Hania,Edraki, Najmeh,Iraji, Aida,Firuzi, Omidreza,Akbarzadeh, Tahmineh
, (2019/02/09)
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
Isoxazole type of model acrosomal enzyme inhibitor and method for preparing same (by machine translation)
-
, (2016/11/21)
The invention relates to a novel acrosin inhibitor, a preparation method and application in preparation of male antifertility drugs thereof. Specifically, the invention relates to a novel acrosin inhibitor shown as formula I, wherein all substituents are defined as the specification. The invention also relates to the preparation method of the acrosin inhibitor and application of the inhibitor in preparation of male antifertility drugs. (formula I).
Design and synthesis of phenylisoxazole derivatives as novel human acrosin inhibitors
Zhao, Juntao,Tian, Wei,Qi, Jingjing,Lv, Diya,Liu, Yang,Jiang, Yan,Dong, Guoqiang,Chen, Qianqian,Zhou, Youjun,Zhu, Ju,Wang, Heling,Sheng, Chunquan,Lv, Jiaguo
, p. 2802 - 2806 (2014/06/10)
Human acrosin is an attractive target for the discovery of novel male contraceptives. Isoxazole derivative ISO-1, a small-molecule weak human acrosin inhibitor, was used as the starting point for lead optimization. After two rounds of structure-based inhibitor design, a highly potent inhibitor B6 (IC50 = 1.44 μM) was successfully identified, which showed good selectivity over trypsin and represents one of the most active human acrosin inhibitors up to date.
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
Reaction of esters of 2-arylcyclo-propanecarboxylic acids with nitrous acid. Synthesis of aryl-substituted 3-ethoxycarbonyl-4,5-dihydroisoxazoles and 3-ethoxycarbonylisoxazoles
Kadzhaeva,Trofimova,Fedotov,Potekhin,Gazzaeva,Mochalov,Zefirov
experimental part, p. 595 - 605 (2010/03/05)
Esters of 2-arylcyclopropanecarboxylic acids react with nitrous acid generated in situ with regioselective insertion of the nitrosyl cation into the cyclopropane ring. Depending on the substrate/nitrosylating agent ratio, the reaction proceeds with the formation of either aryl-substituted 3-ethoxycarbonyl-4,5-dihydroisoxazoles or the corresponding isoxazoles. The nature and position of the substituents in the aromatic ring of the starting 2-arylcyclopropanecarboxylic acid esters affect the reaction rate but have no effect on the regioselectivity of the attack by the nitrosyl cation on the three-membered ring. A dependence of the reactivity of isomeric substrates on their stereochemistry and position of the nitro group in the aromatic ring is noted for 2- and 4-nitrophenyl derivatives of esters of cis- and trans-2-arylcyclopropanecarboxylic acids.
