Details

Autor(en) / Beteiligte

• Bandgar, Babasaheb P.
• Patil, Sachin A.
• Gacche, Rajesh N.
• Korbad, Balaji L.
• Hote, Balwant S.
• Kinkar, Santosh N.
• Jalde, Shivkumar S.

Titel

Synthesis and biological evaluation of nitrogen-containing chalcones as possible anti-inflammatory and antioxidant agents

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2010-01, Vol.20 (2), p.730-733

Ort / Verlag

Amsterdam: Elsevier Ltd

Erscheinungsjahr

2010

Quelle

Elsevier ScienceDirect Journals

Beschreibungen/Notizen

• A novel series of nitrogen-containing chalcones were synthesized and were screened for anti-inflammatory and antioxidant activity. Tested compounds ( 4c, 3b, 4d, 6b) were showed pro-inflammatory enzyme inhibitory activity. Whereas tested compounds ( 7b, 7c, 6c, 4b, 3c, 3b) were observed as effective inhibitors of COX-2. A novel series of nitrogen-containing chalcones were synthesized by Mannich reaction and were screened for anti-inflammatory related activities such as inhibition of cyclooxygenase-2 (COX-2), trypsin and β-glucuronidase. The antioxidant potential was demonstrated using 1,1-diphenyl-2-picryl hydrazine (DPPH) radical scavenging activity. The results of the above studies shows that the compounds synthesized were found to be effective inhibitors of above pro-inflammatory enzymes, and were found to be possess moderate radical scavenging potential. Overall, the results of the studies reveal that the chalcones with N-methyl piperazine methyl and piperidine methyl substitution ( 4c, 3b, 4d, 6b) seems to be important for inhibition of β-glucuronidase. Whereas the chalcones with piperidine methyl substitution ( 8b, 7b, 7c, 6c, 4b, 3c, 3b) were observed as effective inhibitors of COX-2, while the same compounds were found to be less reactive against COX-1 as compared to COX-2.