22179-80-2Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS
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Paragraph 0831-0832, (2021/04/02)
The invention provides new heterocyclic compounds having the general formula (I) wherein A, L1, X, m, n and R1 to R4 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
Design, synthesis, and biological evaluation of 1,2,4-oxadiazole-containing pyrazolo[3,4-b]pyridinones as a new series of AMPKɑ1β1γ1 activators
Xiao, Zhihong,Peng, Yajun,Zheng, Bifeng,Chang, Qi,Guo, Yating,Chen, Zhuo,Li, Qianbin,Hu, Gaoyun
, (2021/03/16)
Adenosine monophosphate-activated protein kinase (AMPK) plays a key role in maintaining whole-body homeostasis and has been regarded as a therapeutic target for the treatment of diabetic nephropathy (DN). Herein, a series of 1,2,4-oxadiazole-containing py
KCNT1 INHIBITORS AND METHODS OF USE
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Paragraph 000390, (2020/11/23)
The present invention is directed to, in part, compounds and compositions useful for preventing and/or treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene (e.g., KCNT1). Methods of treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene such as KCNT1 are also provided herein.
Synthesis and Biological Evaluation of Sigma-1 (σ1) Receptor Ligands Based on Phenyl-1,2,4-oxadiazole Derivatives
Cao, Xudong,Yao, Zhongyuan,Dou, Fei,Zhang, Yifang,Qiu, Yinli,Zhao, Song,Xu, Xiangqing,Liu, Xin,Liu, Bi-Feng,Chen, Yin,Zhang, Guisen
, (2019/02/26)
In this study, a series of phenyl-1,2,4-oxadiazole derivatives were synthesized and evaluated for anti-allodynic activity. Structure–activity relationship studies identified 1-{4-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]butyl}piperidine (39) with excellent affinity for the σ1 receptor and selectivity for the σ2 receptor, with poor activity to other central nervous system neurotransmitter receptors and transporters associated with pain. Compound 39 exhibited dose-dependent efficacy in suppressing the formalin-induced flinching and attenuating mechanical allodynia in chronic constriction injury-induced neuropathic rats. These results suggest that compound 39 exerts potent antihyperalgesic activity and could be considered as a promising candidate for treating neuropathic pain.
A cascade process for directly converting nitriles (RCN) to cyanamides (RNHCN) via SO2F2-activated Tiemann rearrangement
Zhang, Guofu,Zhao, Yiyong,Ding, Chengrong
supporting information, p. 7684 - 7688 (2019/08/30)
A simple, mild and practical process for the direct conversion of nitriles to cyanamides was newly discovered and exhibited a wide substrate scope as well as great functional group-tolerability (36 examples). In this efficient strategy, the in situ generated amidoximes obtained from the reaction of nitriles with hydroxylamine subsequently underwent Tiemann rearrangement, producing the corresponding cyanamides with great isolated yields under SO2F2. Additionally, the control experiments reportedly shed light on the tentative mechanism involved in the formation and elimination of the key intermediate: a sulfonyl ester.
Iron(III) Chloride/l-Proline as an Efficient Catalyst for the Synthesis of 3-Substituted 1,2,4-Oxadiazoles from Amidoximes and Triethyl Orthoformate
Kaboudin, Babak,Kazemi, Foad,Pirouz, Maryam,Khoshkhoo, Aysan Baharian,Kato, Jun-Ya,Yokomatsu, Tsutomu
, p. 3597 - 3602 (2016/10/18)
A general, facile, and efficient method is presented for the synthesis of 3-substituted 1,2,4-oxadiazoles from amidoximes and triethyl orthoformate. The procedure employs an iron(III) chloride/l-proline catalytic system and the 3-substituted 1,2,4-oxadiaz
Mild and efficient one-pot synthesis of 3,5-disubstituted 1,2,4-oxadiazoles from nitriles mediated by K 3PO 4
Movassagh, Barahman,Talebsereshki, Farzaneh
supporting information, p. 188 - 194 (2013/12/04)
Potassium phosphate, K3PO4, has been proved to be a cheap, strong, and efficient reagent for the one-pot synthesis of 3,5-disubstituted-1,2,4-oxadiazoles from nitriles and acid chlorides under mild conditions. [Supplementary material
Formation of aromatic amidoximes with hydroxylamine using microreactor technology
Voeroes, Attila,Baan, Zoltan,Mizsey, Peter,Finta, Zoltan
, p. 1717 - 1726 (2013/01/15)
In this contribution, the application of microreactor technology for amidoxime formation is demonstrated, with different aromatic nitriles reacted with a 50% solution of hydroxylamine (HA) under homogeneous conditions to reach full conversion. All reactio
Organic reactions in water: An efficient method for the synthesis of 1,2,4-oxadiazoles in water
Kaboudin, Babak,Malekzadeh, Leila
supporting information; experimental part, p. 6424 - 6426 (2011/12/22)
A simple and efficient process has been developed for the synthesis of 1,2,4-oxadiazoles in good yields through the reaction of amidoximes with anhydrides under catalyst-free conditions in water.
Clean one-pot synthesis of 1,2,4-oxadiazoles under solvent-free conditions using microwave irradiation and potassium fluoride as catalyst and solid support
Rostamizadeh, Shahnaz,Ghaieni, Hamid Reza,Aryan, Reza,Amani, Ali Mohammad
experimental part, p. 494 - 497 (2010/03/03)
Potassium fluoride was found to be an efficient catalyst and solid support for the synthesis of 3,5-disubstituted-1,2,4-oxadiazoles. In this work, a one-pot method for the synthesis of these compounds from the reaction of nitriles with hydroxylamine hydro
