Abstract
A series of pyrazolo[4,3-c]cinnoline derivatives was synthesized, characterized and evaluated for anti-inflammatory and antibacterial activity. Test compounds that exhibited good anti-inflammatory activity were further screened for their ulcerogenic and lipid peroxidation activity. Compounds 4d and 4l showed promising anti-inflammatory activity with reduced ulcerogenic and lipid peroxidation activity when compared to naproxen. Docking results of these two compounds with COX-2 (PDB ID: 1CX2) also exhibited a strong binding profile. Among the test derivatives, compound 4i displayed significant antibacterial property against gram-negative (Escherichia coli and Pseudomonas aeruginosa) and gram-positive (Staphylococcus aureus) bacteria. However, compound 4b emerged as the best dual anti-inflammatory-antibacterial agent in the present study.
Copyright © 2012 Elsevier Masson SAS. All rights reserved.
MeSH terms
-
Administration, Oral
-
Animals
-
Anti-Bacterial Agents / chemical synthesis*
-
Anti-Bacterial Agents / pharmacology
-
Anti-Inflammatory Agents / chemical synthesis*
-
Anti-Inflammatory Agents / pharmacology
-
Carrageenan
-
Cyclooxygenase 2 / metabolism
-
Edema / chemically induced
-
Edema / drug therapy*
-
Edema / metabolism
-
Escherichia coli / drug effects
-
Escherichia coli / growth & development
-
Heterocyclic Compounds, 2-Ring / chemical synthesis*
-
Heterocyclic Compounds, 2-Ring / pharmacology
-
Inflammation / chemically induced
-
Inflammation / drug therapy*
-
Inflammation / metabolism
-
Lipid Peroxidation / drug effects
-
Microbial Sensitivity Tests
-
Molecular Docking Simulation
-
Naproxen / pharmacology
-
Pseudomonas aeruginosa / drug effects
-
Pseudomonas aeruginosa / growth & development
-
Pyrazoles / chemical synthesis*
-
Pyrazoles / pharmacology
-
Rats
-
Rats, Wistar
-
Staphylococcus aureus / drug effects
-
Staphylococcus aureus / growth & development
-
Structure-Activity Relationship
-
Ulcer / chemically induced
-
Ulcer / pathology
Substances
-
Anti-Bacterial Agents
-
Anti-Inflammatory Agents
-
Heterocyclic Compounds, 2-Ring
-
Pyrazoles
-
Naproxen
-
Carrageenan
-
Cyclooxygenase 2
-
PTGS2 protein, human
-
cinnoline