42191-47-9Relevant academic research and scientific papers
3-(5-)-Amino-o-diarylisoxazoles: Regioselective synthesis and antitubulin activity
Tsyganov, Dmitry V.,Khrustalev, Victor N.,Konyushkin, Leonid D.,Raihstat, Mikhail M.,Firgang, Sergei I.,Semenov, Roman V.,Kiselyov, Alex S.,Semenova, Marina N.,Semenov, Victor V.
, p. 112 - 125 (2014/01/17)
A regioselective synthesis of both 5-amino- and 3-aminodiarylisoxazoles substituted with polyalkoxyaryl pharmacophores has been validated. Starting materials for the synthetic scheme were easily available from plant extracts. The targeted molecules were f
An Efficient Synthesis of 2-Substituted Quinazolin-4(3 H)-ones Catalyzed by Iron(III) Chloride
Mekala, Ramamohan,Akula, Raghunadh,Kamaraju, Raghavendra Rao,Bannoth, Chandrasekhar Kothapalli,Regati, Sridhar,Sarva, Jayaprakash
supporting information, p. 821 - 826 (2014/04/03)
A simple and highly efficient synthesis of 2-substituted quinazolin-4(3H)-ones by the iron(III) chloride catalyzed reaction of isatoic anhydride with various amidoxime derivatives was developed. Several aryl and alkyl amidoximes were screened to demonstra
Synthesis and in vitro antibacterial assessment of novel chromones featuring 1,2,4-oxadiazole
Diwakar, Santosh D.,Joshi, Ratnadeep S.,Gill, Charansing H.
experimental part, p. 882 - 887 (2011/09/16)
Figure represented. In search for a new antibacterial agent with improved antimicrobial spectrum and potency, we designed and synthesized a series of novel 3-((Z)-2-(5-methyl-1,2,4-oxadiazol-3-yl)-2-(4-nitrophenyl)vinyl)-4H- chromen-4-ones (7a-h) by conve
Novel oxadiazole analogues derived from ethacrynic acid: Design, synthesis, and structure - Activity relationships in inhibiting the activity of glutathione S-transferase P1-1 and cancer cell proliferation
Yang, Xinmei,Liu, Guyue,Li, Hongcai,Zhang, Yun,Song, Dandan,Li, Chunmin,Wang, Rui,Liu, Bo,Liang, Wen,Jing, Yongkui,Zhao, Guisen
experimental part, p. 1015 - 1022 (2010/08/06)
Ethacrynic acid (EA) is a glutathione S-transferase P1-1 (GST P1-1) inhibitor with weak antiproliferative ability in tumor cells. By use of the principle of bioisosterism, a series of novel EA oxadiazole analogues were designed and synthesized. The struct
Synthesis and cannabinoid activity of 1-substituted-indole-3-oxadiazole derivatives: Novel agonists for the CB1 receptor
Moloney, Gerard P.,Angus, James A.,Robertson, Alan D.,Stoermer, Martin J.,Robinson, Michael,Wright, Christine E.,McRae, Ken,Christopoulos, Arthur
, p. 513 - 539 (2008/12/21)
An exploratory chemical effort has been undertaken to develop a novel series of compounds as selective CB1 agonists. It is hoped that compounds of this type will have clinical utility in pain control, and cerebral ischaemia following stroke or traumatic head injury. We report here medicinal chemistry studies directed towards the investigation of a series of 1-substituted-indole-3-oxadiazoles as potential CB1 agonists. Crown Copyright
AGENT FOR PREVENTING OR TREATING NEUROPATHY
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Page/Page column 141-142, (2010/02/06)
The present invention provides an agent for preventing or treating neuropathy having superior action and low toxicity. This agent comprises a compound represented by the formula:wherein ring A is a 5-membered aromatic heterocycle containing 2 or more nitrogen atoms, which may further have substituent(s);B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group;X is a divalent acyclic hydrocarbon group;Z is -O-, -S-, -NR2-, -CONR2- or -NR2CO- (R2 is a hydrogen atom or an optionally substituted alkyl group);Y is a bond or a divalent acyclic hydrocarbon group;R1 is an optionally substituted cyclic group, an optionally substituted amino group or an optionally substituted acyl group, provided that when the 5-membered aromatic heterocycle represented by ring A is imidazole, then Z should not be -O-, or a salt thereof.
1,2,4-Oxadiazole derivatives of phenylalanine: potential inhibitors of substance P endopeptidase
Borg, S.,Luthman, K.,Nyberg, F.,Terenius, L.,Hacksell, U.
, p. 801 - 810 (2007/10/02)
The synthesis and the biological activity of a series of benzyl or aryl substituted 1,2,4-oxadiazole derivatives of phenyl-alanine are described.A base-promoted intermolecular cyclization reaction was performed using racemic tert-butyloxycarbonyl protected phenylalanine methyl ester and an amidoxime.After deprotection of the amino function the compounds were evaluated for their affinity to rat brain NK1-receptors and as inhibitors of a specific substance P cleaving enzyme, substance P endopeptidase (SPE), isolated from human cerebrospinal fluid.The results indicate that several compounds are weak inhibitors of SPE.However, all compounds lacked appreciable NK1-receptor affinity.Keywords: 1,2,4-oxadiazoles / substance P endopeptidase / Phe-Phe mimetics / amide bioisostere / NK1-receptor affinity
