306963-82-6Relevant academic research and scientific papers
Synthesis and evaluation of anti-inflammatory, analgesic, ulcerogenicity and nitric oxide-releasing studies of novel ibuprofen analogs as nonulcerogenic derivatives
Sarkate, Aniket P.,Lokwani, Deepak K.,Patil, Ajit A.,Bhandari, Shashikant V.,Bothara, Kailash G.
, p. 795 - 808 (2012/05/31)
Since the last 41 years, Ibuprofen has been one of the most widely used Non-Steroidal Anti-Inflammatory Drug (NSAID) due to its anti-inflammatory actions. As all the NSAIDs are suffering from the deadlier GI toxicities, Ibuprofen also is no exception to these toxicities. The free -COOH group is thought to be responsible for the Gastrointestinal (GI) tract toxicity associated with all the traditional NSAIDs. Therefore, the main aim of this study was to develop new chemical entities as potential anti-inflammatory agents with less GI toxicities. In this article, synthesis of a series of Hybrid molecules containing important pharmacophore of Ibuprofen and substituted diaryl rings on 5-membered heterocycle similar to coxibs and Nitric oxidereleasing moiety are described. All the synthesized compounds were tested in vivo for their anti-inflammatory, analgesic, ulcerogenic properties, and histopathological studies and in vitro for their nitric oxide-releasing properties. Out of the six synthesized compounds, four compounds showed significant anti-inflammatory and analgesic activity which was compared with standard. All the synthesized compounds exhibited significant nitric oxide-releasing and reduced GI ulcerogenic activity. Springer Science+Business Media, LLC 2010.
Synthesis, characterization and biological studies of some bioactive thiazolotriazole derivatives
Kumsi, Manjunatha,Poojary, Boja,Lobo, Prajwal Lourdes,Kumari, Nalilu Suchetha,Chullikana, Anoop
, p. 1509 - 1515 (2011/02/28)
The key precursor rac-2-(4-isobutylphenyl)ethyl-1,2,4-triazole-5-thione (3) was synthesized in good yield from Ibuprofen (1). One-pot three-component reactions of 3 with 5-aryl-furan-2-carboxaldehydes/substituted aromatic aldehydes and monochloroacetic acid in acetic acid in the presence of acetic anhydride and anhydrous sodium acetate afforded substituted thiazolo[3,2-b][1,2, 4]triazole derivatives 4 and 5. The structures of the newly synthesized compounds were elucidated by elemental analyses and spectral data. The compounds were tested for their in-vitro antimicrobial activities.
Synthesis of some fused triazole derivatives containing 4-isobutylphenylethyl and 4-methylthiophenyl moieties
Kumsi, Manjunatha,Poojary, Boja,Lobo, Prajwal L.,Fernandes, Jennifer,Chikkanna, Chandrashekhar
experimental part, p. 1353 - 1358 (2011/01/08)
A series of substituted [1,3]thiazolo[3,2-b][1,2,4]triazole derivatives 4 were synthesized in good yield by condensing 2-substituted-1,2,4-triazole-5- thiols 3 with various N-aryl-maleimides in acetic acid media. All structures of the newly synthesized compounds were elucidated by elemental analyses and spectral data.
6-Benzylidenethiazolo[3,2-b]-1,2,4-triazole-5(6H)-ones substituted with ibuprofen: Synthesis, characterization and evaluation of anti-inflammatory activity
Tozkoparan, Birsen,Goekhan, Nesrin,Aktay, Goeknur,Yesilada, Erdem,Ertan, Mevluet
, p. 743 - 750 (2007/10/03)
In this study, the synthesis of 3-[1-(4-(2-methylpropyl)phenyl)ethyl]- 1,2,4-triazole-5-thione (2) and its condensed derivatives 6- benzylidenethiazolo[3,2-b]-1,2,4-triazole-5(6H)-ones (2a-u) are described. The structures of the compounds were elucidated by spectral and elemental analysis. In the pharmacological studies, anti-inflammatory activities of these compounds have been screened. Among the compounds examined, the compounds 2 and 2g possessed the most prominent and consistent activity. In gastric ulceration studies the synthesized compounds were generally found to be safe at a 200 mg/kg dose level. (C) 2000 Edition scientifique et medicales Elsevier SAS.
