109544-27-6Relevant articles and documents
Synthesis and molecular docking study of new 1,3-oxazole clubbed pyridyl-pyrazolines as anticancer and antimicrobial agents
Katariya, Kanubhai D.,Vennapu, Dushyanth R.,Shah, Shailesh R.
, (2021)
The present investigation is in the quest of some novel biologically potent heterocyclic compounds 1-aryl-3-(2-(4-chlorophenyl)-5-methyl-1,3-oxazol-4-yl)-propenones 6(a-e) and [5-aryl-3-(2-{(4-chlorophenyl)-5-methyl-1,3-oxazol-4-yl)}-4,5-dihydro-1H-pyrazol-1-yl)]-(pyridin-4-yl)methanone 7(a-e) incorporated with biologically active heterocyclic entities namely oxazole, pyrazoline and pyridine. The structures of all the compounds were elucidated using various spectroanalytical techniques such as FT-IR, 1H NMR, 13C NMR and mass spectrometry. The synthesized compounds were studied for their anticancer activity at the National Cancer Institute (NCI, USA) against 60 cancer cell line panel. Data of anticancer activity study revealed that the compound 6(d) has the highest potency. Furthermore, all the compounds were studied for their in vitro antibacterial and antifungal activities. As documented, all the prepared compounds performed well against these pathogenic strains. Moreover, data acquired from the molecular docking studies are very inspiring with respect to the potential utilization of these compounds to help overcome microbe resistance to pharmaceutical drugs.
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.
supporting information, 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.
