93041-44-2Relevant academic research and scientific papers
Design, synthesis and in vitro biological evaluation of isoxazol-4-carboxa piperidyl derivatives as new anti-influenza A agents targeting virus nucleoprotein
Pei, Shuchen,Xia, Shihao,Yang, Fating,Chen, Junlin,Wang, Mengdie,Sun, Wanlin,Li, Ziqiang,Yuan, Kangyao,Chen, Jun
, p. 4446 - 4454 (2020/02/13)
Influenza infection is a major cause of morbidity and mortality during seasonal epidemics and sporadic pandemics. It is important and urgent to develop new anti-influenza agents with a new mechanism of action. Nucleozin has been reported as a potent antagonist of nucleoprotein accumulation in the nucleus. In this study, a new series of isoxazol-4-carboxa piperidyl derivatives 1a-j were synthesized and their chemical structures were confirmed by 1H, 13C NMR and mass spectral data. Furthermore, all the synthesized compounds were evaluated for in vitro anti-influenza virus activity against influenza virus (A/PR/8/34 H1N1). Among all the compounds, 1a, 1b, 1c, 1f and 1g exhibited more potent activity than the standard drug, and compound 1b has showed most promising anti-influenza virus activity. These results are also consistent with the docking study results in terms of the design of compounds targeting influenza A via viral nucleoprotein.
NOVEL PIPERAZINE ANALOGS AS BROAD-SPECTRUM INFLUENZA ANTIVIRALS
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Page/Page column 35, (2012/03/27)
A compound of Formula (I) is set forth, including pharmaceutically acceptable salts thereof, wherein Het is a 5 or 6-membered heterocycle with -N, -O, or -S adjacent to the -Ar substituent or adjacent to the point of attachment for the -Ar substituent; Ar
NOVEL PIPERAZINE ANALOGS WITH SUBSTITUTED HETEROARYL GROUPS AS BROAD-SPECTRUM INFLUENZA ANTIVIRALS
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Page/Page column 32, (2012/04/17)
A compound of the following Formula (I) is set forth, including pharmaceutically acceptable salts thereof: wherein Het is a 5 or 6-membered heterocycle with -N, -O, or -S adjacent to the -Ar substituent or adjacent to the point of attachment for the -Ar substituent; Ar is aryl or heteroaryl; R is -CH3, -CH2F, -CHF2 or -CH=CH2; V is -H, -CH3 or =0; W is -NO2, -CI, -Br, -CH2OH, or -CN; X is -CI, -Br, -F, -CH3, -OCH3, or -CN; Y is -CH or -N; and Z is -CH or -N. This compound is useful in compositions for the prevention and treatment of influenza virus.
An efficient one-pot synthesis of 3-aryl-5-methylisoxazoles from aryl aldehydes
Zhu, Shirong,Shi, Shuhao,Gerritz, Samuel W.
, p. 4001 - 4004 (2011/08/21)
An efficient protocol for the one-pot preparation of alkyl 3-aryl-5-methylisoxazole-4-carboxylates from aryl aldehydes is described. This method is readily amenable to the large scale preparation of isoxazoles as well as the parallel synthesis of isoxazole libraries.
Isoxazolopyridone derivatives as allosteric metabotropic glutamate receptor 7 antagonists
Nakamura, Masayuki,Kurihara, Hideki,Suzuki, Gentaroh,Mitsuya, Morihiro,Ohkubo, Mitsuru,Ohta, Hisashi
scheme or table, p. 726 - 729 (2010/05/18)
This Letter describes the synthesis and evaluation of mGluR7 antagonists in the isoxazolopyridone series. In the course of modification in this class, novel solid support synthesis of the isoxazolopyridone scaffold was developed. Subsequent chemical modification led to the identification of several potent derivatives with improved physicochemical properties compared to a hit compound 1. Among these, 2 showed good oral bioavailability and brain penetrability, suggesting that 2 may be useful for in vivo study to elucidate the role of mGluR7.
Synthesis and structure-activity relationships of isoxazole carboxamides as growth hormone secretagogue receptor antagonists
Xin, Zhili,Zhao, Hongyu,Serby, Michael D.,Liu, Bo,Schaefer, Verlyn G.,Falls, Douglas H.,Kaszubska, Wiweka,Colins, Christine A.,Sham, Hing L.,Liu, Gang
, p. 1201 - 1204 (2007/10/03)
A series of isoxazole carboxamide derivatives has been developed as potent ghrelin receptor antagonists. The synthesis and structure-activity relationship (SAR) are described.
