TY - JOUR
T1 - Synthesis and pharmacological evaluation of pyrazolo[4,3-c]cinnoline derivatives as potential anti-inflammatory and antibacterial agents
AU - Tonk, Rajiv Kumar
AU - Bawa, Sandhya
AU - Chawla, Gita
AU - Deora, Girdhar Singh
AU - Kumar, Suresh
AU - Rathore, Vandana
AU - Mulakayala, Naveen
AU - Rajaram, Azad
AU - Kalle, Arunasree M.
AU - Afzal, Obaid
PY - 2012/11
Y1 - 2012/11
N2 - 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.
AB - 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.
KW - Anti-inflammatory agent
KW - Antibacterial agent
KW - COX-2 inhibitors
KW - Docking simulations
KW - Pyrazolo[4,3-c]cinnoline
KW - Ulcerogenic activity
UR - https://www.scopus.com/pages/publications/84867085510
U2 - 10.1016/j.ejmech.2012.08.045
DO - 10.1016/j.ejmech.2012.08.045
M3 - Article
C2 - 23059546
AN - SCOPUS:84867085510
SN - 0223-5234
VL - 57
SP - 176
EP - 184
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
ER -