50511-87-0Relevant academic research and scientific papers
Antiinflammatory and Antiproliferative Activity of Naphthoxazole, Fused Hetero-benzoxazole and Bridged Benzobicyclic Photoproducts
?agud, Ivana,Ratkovi?, Ana,Cedilak, Matea,Zlatar, Ivo,Bosnar, Martina,Kelava, Vanja,?kori?, Irena
, p. 191 - 201 (2019)
Biological activity of naphthoxazoles, fused hetero-benzoxazoles and benzobicyclo[3.2.1]-derivatives was investigated in proliferation and inflammation based assays. The tested compounds were prepared by photocylization or photocycloaddition reactions. Effect of compounds on proliferation of several cancer cell lines was determined by measuring cell metabolic activity through time. Lipopolysaccharide (LPS) stimulation of peripheral blood mononuclear cells (PBMC) was used to investigate antiinflammatory properties of the compounds. Several naphthoxazoles and fused hetero-benzoxazoles inhibited TNFα protein expression in LPS stimulated PBMC, indicating possible antiinflammatory role which would be interesting to further investigate. Physico-chemical properties of tested compounds have been also studied using chromatographic lipophilicity measure, chrom logD and logP was calculated as the importance of physico-chemical properties of compounds at early stage of discovery of new drugs is well established. The similarities in structure and activity of some representative compounds affirm the need to further address their antiinflammatory properties.
Naphthoxazoles and heterobenzoxazoles: Cholinesterase inhibition and antioxidant activity
?agud, Ivana,?kori?, Irena,Bur?ul, Franko
, p. 118 - 124 (2019/05/16)
Finding novel cholinesterase inhibitors that would be able to cross the blood–brain barrier, have favorable pharmacokinetic parameters, and reduce hepatotoxicity along with other side effects has been the main focus of investigations dealing with Alzheimer disease. In this study we evaluated cholinesterase inhibitory and antioxidant activity of seven oxazole derivatives. These compounds have been efficiently and sustainably prepared by photochemical electrocy-clization reaction. Various naphthoxazoles have been previously investigated as potential antibacterial, antituberculosis, and anticancer agents. They have also been tested for antioxidant activity, but never for cholinesterase inhibitory activity. Among the tested oxazole derivatives, fused heterobenzoxazole compounds with pyridine and thiophene moiety, oxazolo[5,4-h]isoquinoline, thieno[2’,3’:5,6]benzo[1,2-d]oxazole, and thieno[3’,2’:5,6]benzo[1,2-d]oxazole, showed the greatest potential for both cholinesterase inhibitory and antioxidant activity. Among them, thieno[2’,3’:5,6]benzo[1,2d]oxazole was found to be the best one.
Photochemical approach to naphthoxazoles and fused heterobenzoxazoles from 5-(phenyl/heteroarylethenyl)oxazoles
Sagud, Ivana,Faraguna, Fabio,Marinic, Zeljko,Sindler-Kulyk, Marija
experimental part, p. 2904 - 2908 (2011/05/28)
A new synthetic approach is presented for the synthesis of naphthoxazoles and fused heterobenzoxazoles. The starting 5-(aryl/furyl/thienyl/pyridyl ethenyl)oxazoles are prepared from the corresponding α,β-unsaturated aldehydes using Van Leusen reagent in v
