Synthesis and biological evaluation of some pyrazolylpyrazolines as anti-inflammatory-antimicrobial agents.
A new series of pyrazolylpyrazolines (5a-k) was synthesized by the reaction of appropriate chalcones (3a-k) with 4-hydrazinobenzenesulfonamide hydrochloride (4) in ethanol. All the newly synthesized target compounds (5a-k) were screened for their anti-inflammatory activity using carrageenan-induced rat paw edema assay. Compounds 5g and 5j showed pronounced anti-inflammatory activity comparable to the reference standard nimesulide, whereas, compounds 5b, 5d and 5h displayed good anti-inflammatory activity. Additionally, the synthesized compounds were evaluated for their in vitro antimicrobial activity against two Gram-positive bacteria and two Gram-negative bacteria. Four compounds 5c, 5h-5j showed good broad spectrum activity against all the tested Gram-positive and Gram-negative bacterial strains. Compound 5j could be identified as the most biologically active member within this study with an interesting dual anti-inflammatory and antibacterial profile.
Sharma
Pawan K
PK
Department of Chemistry, Kurukshetra University, Kurukshetra-136 119, Haryana, India. talk2pawan@gmail.com
Kumar
Satish
S
Kumar
Pawan
P
Kaushik
Pawan
P
Kaushik
Dhirender
D
Dhingra
Yogita
Y
Aneja
Kamal R
KR
D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D001419:Bacteria / Q000187:drug effects; D004487:Edema / Q000188:drug therapy; D008297:Male; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D017208:Rats, Wistar
D000890:Anti-Infective Agents; D000893:Anti-Inflammatory Agents; D011720:Pyrazoles