Synthesis, analgesic and anti-inflammatory activities of some novel pyrazolines derivatives

• Published in: Bioorganic & medicinal chemistry letters Vol. 20; no. 12; pp. 3721 - 3725
• Main Authors: Joshi, Ratnadeep S., Mandhane, Priyanka G., Diwakar, Santosh D., Dabhade, Sanjay K., Gill, Charansingh H.
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier Ltd 15.06.2010; Elsevier
• Subjects: Analgesic; Analgesics; Analgesics - chemical synthesis; Analgesics - pharmacology; Animals; Anti-inflammatory activity; Anti-Inflammatory Agents - chemical synthesis; Anti-Inflammatory Agents - pharmacology; Biological and medical sciences; Bones, joints and connective tissue. Antiinflammatory agents; Diclofenac; Drug Design; Edema - chemically induced; Edema - drug therapy; Hydrazines; Medical sciences; Mice; N-phenylpyrazol-1-carbothioamide; Neuropharmacology; Pain - chemically induced; Pain - drug therapy; Pharmacology. Drug treatments; Pyrazoles - chemical synthesis; Pyrazoles - pharmacology; Pyrazolines; Rats; Anti-inflammatory activity; Analgesic; N-phenylpyrazol-1-carbothioamide; Pyrazolines; Rat; Thiosemicarbazone; Rodentia; Antiinflammatory agent; Morpholine derivatives; Biological activity; Diclofenac; Vertebrata; Mammalia; Mouse; Thioamide; Animal; Pyrazole derivatives; Phenols; Chemical synthesis
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2010.04.082

In search for a new analgesic and anti-inflammatory agent with improved potency, we designed and synthesized a series of 3,2-(4,5-dihydro-5-(4-morphilinophenyl)-1H-pyarazol-3-yl)phenols 6(a–g) and its N-phenylpyrazol-1-carbothioamide 7(a–g) by Claisan–Schmidt condensation followed by the reaction of hydrazine hydrate. All the synthesized compounds were assayed for their in vivo analgesic and anti-inflammatory activities. All the compounds synthesized showed the potential to demonstrate analgesic and anti-inflammatory activity, of particular interest compounds 6a, 6b, 6g, 7a, 7d and 7g were found comparable to Diclofenac. In search for a new analgesic and anti-inflammatory agent with improved potency, we designed and synthesized a series of 3,2-(4,5-dihydro-5-(4-morphilinophenyl)-1H-pyarazol-3-yl)phenols 6(a–g) and its N-phenylpyrazol-1-carbothioamide 7(a–g) by Claisan–Schmidt condensation followed by the reaction of hydrazine hydrate. All the synthesized compounds were assayed for their in vivo analgesic and anti-inflammatory activities. All the compounds synthesized showed the potential to demonstrate analgesic and anti-inflammatory activity, of particular interest compounds 6a, 6b, 6g, 7a, 7d and 7g were found comparable to Diclofenac.