124040-00-2Relevant academic research and scientific papers
Design and synthesis of some pyrazole derivatives of expected anti-inflammatory and analgesic activities
Abd-El Gawad, Nagwa M.,Hassan, Ghaneya S.,Georgey, Hanan Hanna
experimental part, p. 983 - 994 (2012/07/31)
Design and synthesis of some pyrazole derivatives 4-11 of expected anti-inflammatory and analgesic activities. In addition, docking of the tested compounds into cyclooxygenase II using (MOE) was performed to rationalize the obtained biological results and their mechanism of action. The structures of the new compounds were elucidated by spectral and elemental analyses. All the newly synthesized compounds were evaluated for their anti-inflammatory activity using the carrageenan-induced rat paw edema method. Analgesic activity of the target compounds was measured using the p-benzoquinone writhing-induced method, and their ability to induce gastric toxicity was also evaluated. Results showed that the newly synthesized compounds exhibited weak to good activities compared to ibuprofen and celecoxib as reference drugs. Some compounds, such 4a and 11b exhibited significant anti-inflammatory activity with gastric ulcerogenic potential less than that of ibuprofen. Results of the analgesic activity showed that compounds possessing good anti-inflammatory activity showed also good analgesic. Substitution of pyrazole ring with at least one aryl moiety was found to be essential for anti-inflammatory and analgesic activities. Free NH (of pyrazole ring) and/or acidic group (COOH) will improve the anti-inflammatory activity. Springer Science+Business Media, LLC 2011.
Some novel observations on ethoxymethylation of 2-hydroxy- and 2-methoxyphenyl benzyl ketones: Isolation of α-methylene- and α-hydroxymethyl derivatives
Jain, Amolak C.,Nayyar, Naresh K.,Paliwal, Poonam
, p. 10 - 14 (2007/10/02)
Ethoxymethylation of benzyl 2-hydroxyphenyl ketones (6a, 6b and 6c) with two mol equivalents of ethoxymethyl chloride in the presence of K2CO3 and DMF affords directly the isoflavanones (8a, 8b, and 8c respectively) albeit in smaller yields than recorded earlier .In the case of 6a and 6b, α-methylene derivatives (7a and 9) are also formed.However, ethoxymethylation of benzyl-2-methoxyphenyl ketones (10a, 10b and 10c) with one mol equivalent of ethoxymethyl chloride under similar conditions gives invariably the α-methylene derivatives (11a, 11b and 11c respectively) and α-hydroxymethyl derivative (12).
