515883-91-7Relevant academic research and scientific papers
Non-carboxylic analogues of arylpropionic acids: Synthesis, anti-inflammatory activity and ulcerogenic potential
Metwally, Kamel A.,Yaseen, Shada H.,Lashine, El-Sayed M.,El-Fayomi, Hassan M.,El-Sadek, Mohamed E.
, p. 152 - 160 (2007)
Two series of 1,2,4-triazoles and 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles derived from three selected arylpropionic acids namely, ibuprofen, flurbiprofen and naproxen, were synthesized and evaluated for anti-inflammatory activity and ulcerogenic potentia
Ibuprofen triazole thiol derivative and application thereof in preparation of novel coronavirus inhibitor
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Paragraph 0079-0081; 0083, (2021/12/07)
The invention relates to an ibuprofen triazole thiol derivative or ibuprofen trithione derivative represented by structural formula I or II. The invention discloses a preparation method, a pharmaceutical composition and application thereof in preparation
Synthesis and Evaluation of Some Phenyl Substituted Azetidine Containing 1, 2, 4-triazole Derivatives as Antibacterial Agents
Dhall, Esha,Jain, Sonika,Mishra, Achal,Dwivedi, Jaya,Sharma, Swapnil
, p. 2859 - 2869 (2018/11/10)
A novel series of phenyl substituted azetidine containing 1, 2, 4-triazole derivatives 7(a–j) were synthesized and characterized by IR, 1HNMR, 13CNMR, and mass spectroscopy. Synthesized 1, 2, 4-triazole derivatives were subsequently assayed in vitro to investigate their antibacterial activity against Staphylococcus aureus, Pseudomonas aeruginosa, and Escherichia coli using broth dilution method. Compounds 7c, 7d, and 7e exhibited potent inhibitory activities as compared to standard cefotaxime. Further, fluorescence spectral studies were also carried out to ascertain the antibacterial potential of compound 7c against two bacterial strains, that is, P.?aeruginosa and S.?aureus. In docking studies, all the compounds exhibited good docking scores between ?12.04 and ?11.36?kcal/mol and indicated that compounds could act through inhibition of bacterial DNA gyrase (PDB ID 3U2D). Among all, 7c has shown the maximum docking score and found in agreement to in vitro studies. In conclusion, synthesized 1, 2, 4-triazole derivatives holds substantial caliber to be categorized as antibacterial agents.
Microwave-mediated synthesis of triazolothiadiazoles as anti-inflammatory, analgesic, and anti-oxidant agents
Sujith,Kalluraya, Balakrishna,Adhikari, Adithya,Vijayanarayana
experimental part, p. 543 - 551 (2012/08/07)
Efficient approach to the synthesis of a series of triazolothiadiazole analogs of ibuprofen has been carried out using microwave energy. Thus a series of 1,2,4-triazolo[3,4-b]-thiadiazoles 5 were synthesized starting from 4-amino-3-[1-(4-isobutylphenyl)ethyl]-5-mercapto-1,2,4-triazole 3 and different aromatic acids using phosphorous oxychloride as cyclizing agent by microwave and conventional method. Microwave irradiation reduces both time and reaction endeavors along with reduced amount of phosphorous oxychloride. In addition, preliminary results of the biological evaluation of these compounds are also reported and they found to exhibit significant antioxidant, anti-inflammatory, and analgesic activities with reduced ulcerogenicity. Springer Science+Business Media, LLC 2011.
Regioselective reaction: Synthesis, characterization and pharmacological activity of some new Mannich and Schiff bases containing sydnone
Nithinchandra,Kalluraya,Aamir,Shabaraya
experimental part, p. 597 - 604 (2012/09/11)
A novel series of 1-substituted aminomethyl-3-[1-(4-isobutylphenyl)ethyl]- 4-(3-aryl-4-sydnonylidene) amino-1,2,4-triazol-5-thiones (9), was prepared from the 3-[1-(4-isobutylphenyl)ethyl]-4-(3-aryl-4-sydnonylidene) amino 5-mercapto-1,2,4-triazoles (8) by aminomethylation with formaldehyde and secondary amine. The structures of Schiff bases (8) and Mannich bases (9) were characterized on the basis of IR, NMR, mass spectra1 data and elemental analysis. The newly synthesized compounds were screened for their anti-inflammatory and analgesic activities. Mannich bases (9) carrying piperidine and morpholine residues showed promising anti-inflammatory and analgesic activity.
Regioselective reaction: Synthesis and pharmacological study of Mannich bases containing ibuprofen moiety
Sujith,Rao, Jyothi N.,Shetty, Prashanth,Kalluraya, Balakrishna
experimental part, p. 3697 - 3702 (2009/11/30)
A series of 4-[(4-aryl)methylidene]amino-2-(substituted-4-ylmethyl)-5-{1-[4-(2-methylpropyl)phenyl]ethyl}-2,4-dihydro-3H-1,2,4-triazole-3-thione (6) were synthesized from an arylpropionic acid namely, ibuprofen by a three-component Mannich reaction. Amino
Condensed bridgehead nitrogen heterocyclic system: Synthesis and pharmacological activities of 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives of ibuprofen and biphenyl-4-yloxy acetic acid
Amir,Kumar, Harish,Javed
, p. 2056 - 2066 (2008/12/23)
Several 3,6-disubstituted-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles were prepared by condensation of 4-amino-5-substituted-3-mercapto-(4H)-1,2,4-triazoles (3a,b) with various substituted aromatic acids and aryl/alkyl isothiocyanates through a one-pot reac
