Analgesic and anti-inflammatory activities of several 4-substituted-6-(3'-nitrophenyl)pyridazin-(2H)-3-one derivatives

Anita Singh,Lakshmayya Lakshmayya,Mohammad Asif

doi:10.1590/s1984-82502013000400030

Anita Singh, Lakshmayya Lakshmayya + Show 1 more

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https://doi.org/10.1590/s1984-82502013000400030

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Abstract

Several 6-aryl-4-substituted benzylidene/furfurylidene pyridazin(2H)-3-one derivatives (4a-f) were synthesized and evaluated as analgesic and anti-inflammatory agents in mice and rats, respectively. All compounds were tested by using Eddy's hot plate and the carrageenan-induced hind paw oedema method for the evaluation of analgesic and anti-inflammatory activities, respectively. Results showed that compounds 4f, 4b, 4d, and 4e exhibited higher analgesic and anti-inflammatory activities than other remaining compounds. All title compounds (4a-f) were characterized by IR, NMR and Mass spectroscopy.

Highlights

The classical non-steroidal anti-inflammatory drugs (NSAIDs) are useful for the treatment of inflammation, pain and fever
The actions of NSAIDs are based on the inhibition of the enzyme cyclooxygenase (COX), which catalyzes the metabolism arachidonic acid (AA) to prostaglandin H2 (PGH2)
PGH2 is further metabolized to prostanoids, prostaglandins (PGs) and thromboxane-A2 (TXA2)

Summary

Introduction

The classical non-steroidal anti-inflammatory drugs (NSAIDs) are useful for the treatment of inflammation, pain and fever. The actions of NSAIDs are based on the inhibition of the enzyme cyclooxygenase (COX), which catalyzes the metabolism arachidonic acid (AA) to prostaglandin H2 (PGH2). PGH2 is further metabolized to prostanoids, prostaglandins (PGs) and thromboxane-A2 (TXA2). Various physiological effects of PGs include acute and chronic inflammatory reactions, blood pressure (BP) change, platelet aggregation, induction of labor and intensification of pain and fever. Among the various pyridazine compounds, 3-amino-6-methyl-pyridazine-4-thiol (ES-1007) (1) is marketed in Germany (Pyridazine analogue) and 4-ethoxy2-methyl-5-morpholino-3(2H)-pyridazinone (emorfazone) (1) is being marketed as pentoil and nandron in Japan as an analgesic and anti-inflammatory drug (Rubat, et al, 1992, Pinna et al, 1992; Flouzat et al, 1993)

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