Synthesis and pharmacological evaluation of pyrazolo[4,3-c]cinnoline derivatives as potential anti-inflammatory and antibacterial agents

Rajiv Kumar Tonk; Sandhya Bawa; Gita Chawla; Girdhar Singh Deora; Suresh Kumar; Vandana Rathore; Naveen Mulakayala; Azad Rajaram; Arunasree M. Kalle; Obaid Afzal

doi:10.1016/j.ejmech.2012.08.045

Synthesis and pharmacological evaluation of pyrazolo[4,3-c]cinnoline derivatives as potential anti-inflammatory and antibacterial agents

Rajiv Kumar Tonk, Sandhya Bawa, Gita Chawla, Girdhar Singh Deora, Suresh Kumar, Vandana Rathore, Naveen Mulakayala, Azad Rajaram, Arunasree M. Kalle, Obaid Afzal

Research output: Contribution to journal › Article › peer-review

68 Scopus citations

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.

Original language	English
Pages (from-to)	176-184
Number of pages	9
Journal	European Journal of Medicinal Chemistry
Volume	57
DOIs	https://doi.org/10.1016/j.ejmech.2012.08.045
State	Published - Nov 2012
Externally published	Yes

Keywords

Anti-inflammatory agent
Antibacterial agent
COX-2 inhibitors
Docking simulations
Pyrazolo[4,3-c]cinnoline
Ulcerogenic activity

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10.1016/j.ejmech.2012.08.045

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Tonk, R. K., Bawa, S., Chawla, G., Deora, G. S., Kumar, S., Rathore, V., Mulakayala, N., Rajaram, A., Kalle, A. M., & Afzal, O. (2012). Synthesis and pharmacological evaluation of pyrazolo[4,3-c]cinnoline derivatives as potential anti-inflammatory and antibacterial agents. European Journal of Medicinal Chemistry, 57, 176-184. https://doi.org/10.1016/j.ejmech.2012.08.045

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title = "Synthesis and pharmacological evaluation of pyrazolo[4,3-c]cinnoline derivatives as potential anti-inflammatory and antibacterial agents",

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.",

keywords = "Anti-inflammatory agent, Antibacterial agent, COX-2 inhibitors, Docking simulations, Pyrazolo[4,3-c]cinnoline, Ulcerogenic activity",

author = "Tonk, \{Rajiv Kumar\} and Sandhya Bawa and Gita Chawla and Deora, \{Girdhar Singh\} and Suresh Kumar and Vandana Rathore and Naveen Mulakayala and Azad Rajaram and Kalle, \{Arunasree M.\} and Obaid Afzal",

year = "2012",

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doi = "10.1016/j.ejmech.2012.08.045",

language = "English",

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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

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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

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SN - 0223-5234

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SP - 176

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JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

Synthesis and pharmacological evaluation of pyrazolo[4,3-c]cinnoline derivatives as potential anti-inflammatory and antibacterial agents

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Keywords

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