351468-59-2Relevant academic research and scientific papers
Design and synthesis of novel 2-phenyl-5-(1,3-diphenyl-1H-pyrazol-4-yl)-1, 3,4-oxadiazoles as selective COX-2 inhibitors with potent anti-inflammatory activity
Bansal, Sumit,Bala, Manju,Suthar, Sharad Kumar,Choudhary, Shivani,Bhattacharya, Shoumyo,Bhardwaj, Varun,Singla, Sumit,Joseph, Alex
, p. 167 - 174 (2014/05/20)
A novel series of 2-phenyl-5-(1,3-diphenyl-1H-pyrazol-4-yl)-1,3,4- oxadiazoles were designed and synthesized for selective COX-2 inhibition with potent anti-inflammatory activity. Among the compounds tested, 9g (2-(3-(4-nitrophenyl)-1-phenyl-1H-pyrazol-4-yl)-5-phenyl-1,3,4-oxadiazole) was found to be the most potent inhibitor of COX-2 with IC of 0.31 μM showing promising degree of anti-inflammatory activity in the carrageenan-induced rat paw edema model with ED of 74.3 mg/kg. The lead compound 9g further showed suppression of acetic acid-induced writhes comparable to that of aspirin and gastro-sparing profile superior to the aspirin. Molecular docking analysis displayed higher binding affinity of ligands towards COX-2 than COX-1.
Hypervalent iodine(III) mediated synthesis of novel unsymmetrical 2,5-disubstituted 1,3,4-oxadiazoles as antibacterial and antifungal agents
Prakash, Om,Kumar, Manoj,Kumar, Rajesh,Sharma, Chetan,Aneja
experimental part, p. 4252 - 4257 (2010/09/16)
A series of novel 2,5-disubstituted 1,3,4-oxadiazoles 4 have been conveniently synthesized by oxidative cyclization of pyrazolylaldehyde N-acylhydrazones 3 promoted by iodobenzene diacetate under mild conditions (11 examples, up to 92% isolated yields). All the eleven compounds were tested in vitro for their antibacterial activity against Gram-positive bacteria namely, Staphylococcus aureus, Bacillus subtilis and two Gram-negative bacteria namely, Escherichia coli and Pseudomonas aeruginosa. All the synthesized compounds were also tested for their inhibitory action against two strains of fungus. A series of novel 2,5-disubstituted 1,3,4-oxadiazoles 4 have been conveniently synthesized by oxidative cyclization of pyrazolylaldehyde N-acylhydrazones 3 promoted by iodobenzene diacetate under mild conditions (11 examples, up to 92% isolated yields).
Synthesis of novel 3-acetyl-2-aryl-5-(3-aryl-1-phenyl-pyrazol-4-yl)-2,3-dihydro-1,3,4-oxadiazoles
Li, Cun-Kui,Ma, Yu-Jie,Cao, Ling-Hua
scheme or table, p. 182 - 185 (2010/04/26)
A series of novel pyrazolyl-substituted 1,3,4-oxadiazole derivatives (4a-4o) were prepared by cyclization of the intermediate N′ -((3-aryl-l-phenyl-pyrazol-4-yl)methylene)arylhydrazide with acetic anhydride. The structures of the new compounds were confir
