Synthesis and Biological Evaluation of Some N‐Arylpyrazoles and Pyrazolo[3, 4‐d]pyridazines as Anti‐Inflammatory Agents. Issue 9 (23rd August 2013)

• Record Type: Journal Article
• Authors: El‐Sabbagh, Osama I.; Mostafa, Samia; Abdel‐Aziz, Hatem A.; Ibrahim, Hany S.; Elaasser, Mahmoud M.
• Is Part Of: Archiv der Pharmazie. Volume 346:Issue 9(2013:Sep.)
• Page Start: 688
• Page End: 698
• Publication Date: 2013-08-23
• Subjects: Pharmaceutical chemistry -- Periodicals; Pharmacology -- Periodicals; 615.19
• DOI: 10.1002/ardp.201300193
• Languages: English
• ISSNs: 0365-6233

Abstract

<abstract abstract-type="main" xml:lang="en"> <title> <x xml:space="preserve">Abstract</x> </title> <sec id="ardp201300193-sec-0001" sec-type="section"> <p>A series of 3, 4‐bis‐chalcone‐<italic>N</italic>‐arylpyrazoles <bold>3a</bold>–<bold>k</bold> was prepared from diacetyl pyrazoles <bold>2a</bold>–<bold>e</bold>. The reaction of <bold>2d</bold> and <bold>2e</bold> with hydrazine hydrate gave pyrazolo[3, 4‐<italic>d</italic>]pyridazine derivatives <bold>4a–b</bold>. Furthermore, the reaction of <bold>2a</bold>–<bold>e</bold> with thiosemicarbazide afforded pyrazolo[3, 4‐<italic>d</italic>]pyridazine thiocyanate salts <bold>5a</bold>–<bold>e</bold>. The synthesized compounds were subjected to <italic>in vivo</italic> anti‐inflammatory and ulcerogenic activity measurements, in addition to determination of their <italic>in vitro</italic> COX selectivity, to give a full profile about their anti‐inflammatory activities. Compounds <bold>3c</bold>, <bold>3f</bold>, <bold>3i</bold>, and <bold>3e</bold> showed significant anti‐inflammatory activity among the synthesized compounds. Moreover, docking studies were performed to give an explanation for their anti‐inflammatory activity through COX selectivity.</p> </sec> </abstract>