867176-56-5Relevant academic research and scientific papers
Synthesis and characterization of flurbiprofen hydrazide derivatives as potential anti-HCV, anticancer and antimicrobial agents
Cikla, Pelin,Tatar, Esra,Kuecuekguezel, Ilkay,Sahin, Fikrettin,Yurdakul, Dilsad,Basu, Amartya,Krishnan, Ramalingam,Nichols, Daniel Brian,Kaushik-Basu, Neerja,Kuecuekguezel, S. Gueniz
, p. 5685 - 5699 (2013)
A novel series of new flurbiprofen hydrazide derivatives 2-(2-fluorobiphenyl-4-yl)-N′-[(substituted phenyl/5-nitro-2-furyl) methylene]propanehydrazide (3a-k), 2-(2-fluorobiphenyl-4-yl)-N-(2-substituted-4- oxo-1,3-thiazolidine-3-yl)propanamide (4a-b, 4d-k), 2-[2-(2-fluorobiphenyl-4-yl) propanoyl]-N-substituted hydrazinecarbothioamide (5a-h) and 2-(2-fluorobiphenyl-4-yl)-N′-[(3-methyl-4-oxo-1,3-thiazolidin-2-ylidene] propanehydrazide (6a-b, 6e and 6g) has been synthesized in this study. All synthesized compounds were screened for antimicrobial activity against various bacterial and fungal strains. Additionally, compounds were evaluated for the ability to inhibit Hepatitis C virus NS5B polymerase. The most active 4-thiazolidinone compound was 4k (SGK119) with 67.0 % and thiosemicarbazide compound was 5d (SGK123) with 69.50 % inhibition at 200 μM against hepatitis C virus NS5B RNA polymerase. Anticancer activity of the selected compounds (3i, 3j, 3h, 4d, 4i and 6b) was determined at a single dose towards the full panel of 60 human cancer cell lines by the National Cancer Institute (NCI). 2-(2-Fluoro-4-biphenylyl)-N-[2-[4-(trifluoromethyl)phenyl]-4-oxo-1, 3-thiazolidine-3-yl]propanamide 4d, containing thiazolidinone ring, demonstrated the most marked effect with 20.80 % growth percent on leukaemia cancer cell line SR at 10-5 M. The results demonstrated that none of the compounds tested have anticandidal and antifungal activities, but two of them (4a and 4i) showed antibacterial inhibition against Micrococcus luteus, and Staphylococcus cohnii and Staphylococcus aureus, respectively.
Synthesis of some new 2-(2-fluoro-4-biphenylyl)propionic acid derivatives as potential anti-inflammatory agents
Amir, Mohammad,Kumar
, p. 175 - 180 (2007/10/03)
The synthesis of a group of 1,3,4-oxadiazoles, 1,2,4-triazoles, 1,3,4-thiadiazoles and 1,2,4-triazine derived from 2-(2-fluoro-4-biphenylyl) propionic acid is described. The structures of new compounds are supported by IR, 1H NMR and MS data. These compounds were tested in vivo for their anti-inflammatory activity. The compounds which showed activity comparable to the standard drug flurbiprofen, were screened for their analgesic, ulcerogenic and lipid peroxidation activities. Five out of seventeen new compounds, showed very good anti-inflammatory activity in the carrageenan induced rat paw edema test with negligible ulcerogenic action. The compounds, which showed less ulcerogenic action, also showed reduced malondialdehyde production (MDA), which is one of the byproducts of lipid peroxidation. The study showed that the compounds inhibit the induction of gastric mucosal lesions and it can be suggested from our results that their protective effects may be related to an inhibition of lipid peroxidation in the gastric mucosa.
