137090-44-9Relevant academic research and scientific papers
1,3-Oxazole-isoniazid hybrids: Synthesis, antitubercular activity, and their docking studies
Katariya, Kanubhai D.,Shah, Shailesh R.
, (2020/01/25)
A series of novel N′-([2-aryl-5-methyl-1,3-oxazole-4-yl]methylene)isonicotino/nicotino hydrazides 10a-l were prepared by the condensation reaction of 2-aryl-5-methyl-1,3-oxazole-4-carbaldehydes 8a-f with the corresponding isonicotino/nicotino hydrazides 9
Development of an Aryloxazole Class of Hepatitis C Virus Inhibitors Targeting the Entry Stage of the Viral Replication Cycle
He, Shanshan,Li, Kelin,Lin, Billy,Hu, Zongyi,Xiao, Jingbo,Hu, Xin,Wang, Amy Q.,Xu, Xin,Ferrer, Marc,Southall, Noel,Zheng, Wei,Aubé, Jeffrey,Schoenen, Frank J.,Marugan, Juan J.,Liang, T. Jake,Frankowski, Kevin J.
, p. 6364 - 6383 (2017/08/02)
Reliance on hepatitis C virus (HCV) replicon systems and protein-based screening assays has led to treatments that target HCV viral replication proteins. The model does not encompass other viral replication cycle steps such as entry, processing, assembly and secretion, or viral host factors. We previously applied a phenotypic high-throughput screening platform based on an infectious HCV system and discovered an aryloxazole-based anti-HCV hit. Structure-activity relationship studies revealed several compounds exhibiting EC50 values below 100 nM. Lead compounds showed inhibition of the HCV pseudoparticle entry, suggesting a different mode of action from existing HCV drugs. Hit 7a and lead 7ii both showed synergistic effects in combination with existing HCV drugs. In vivo pharmacokinetics studies of 7ii showed high liver distribution and long half-life without obvious hepatotoxicity. The lead compounds are promising as preclinical candidates for the treatment of HCV infection and as molecular probes to study HCV pathogenesis.
SUBSTITUTED ACID DERIVATIVES USEFUL AS ANTIDIABETIC AND ANTIOBESITY AGENTS AND METHOD
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Page/Page column 29, (2010/11/29)
Compounds are provided which have the structure of Formula (I): wherein R is hydrogen or C1-C4 alkyl; and each of R1 and R2 is independently hydrogen, C1-C4 alkyl, halo or C1-Cs
Process for the preparation of the PPAR alpha agonist NS-220
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Page/Page column 6, (2010/11/28)
The present invention is concerned with a novel process for the preparation of compounds of formula (I) wherein R1 and R2 are as defined in the description and claims. The compounds of formula (I) are pharmaceutically active substanc
METHOD FOR THE PRODUCTION OF OXAZOLES BY CONDENSING AROMATIC ALDEHYDES WITH A-KETOXIMES TO N-OXIDES AND THEN REACTING THE SAME WITH ACTIVATED ACID DERIVATIVES
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Page/Page column 18, (2008/06/13)
Disclosed is a method for producing oxazoles of formula IV by condensing aromatic aldehydes with a-ketoximes to N-oxides and then reacting the same with activated acid derivatives. The invention relates to a method for producing oxazoles by condensing ald
Hypoglycemic thiazolidinedione derivatives
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, (2008/06/13)
Hypoglycemic thiazolidine-2,4-derivatives STR1 wherein the dotted line represents a bond or no bond; V is --CH=CH--, --N=CH--, --CH=N-- or S; W is CH2, CHOH, CO, C=NOR or --CH=CH--; X is S, O, NR1, --CH=N-- or --N=CH--; Y is CH or N; Z is hydrogen, (C1 -C7)alkyl, (C3 -C7)cycloalkyl, phenyl, naphtyl, pyridyl, furyl, thienyl or phenyl mono- or disubstituted with the same or different groups which are (C1 -C3)alkyl, trifluoromethyl, (C1 -C3)alkoxy, fluoro, chloro or bromo; Z1 is hydrogen or (C1 -C3)alkyl; R is hydrogen or methyl; and n is 1, 2 or 3; a pharamceutically acceptable cationic salt thereof; or a pharmaceutically acceptable acid addition salt thereof when the compound contains basic nitrogen.
