Design and Synthesis of 2-Phenoxynicotinic Acid Hydrazides as Anti-inflammatory and Analgesic Agents.
Summary of "Design and Synthesis of 2-Phenoxynicotinic Acid Hydrazides as Anti-inflammatory and Analgesic Agents."
A series of 2-phenoxynicotinic acid hydrazides were synthesized and evaluated for their analgesic and anti-inflammatory activities. Several compounds having an unsubstituted phenyl/4-pyridyl or C-4 methoxy substituent on the terminal phenyl ring showed moderate to high analgesic or anti-inflammatory activity in comparison to mefenamic acid as the reference drug. The compounds with highest anti-inflammatory activity were subjected to in vitro COX-1/COX-2 inhibition assays and showed moderate to good COX-1 and weak COX-2 inhibition activities.
Affiliation
Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran.
Journal Details
This article was published in the following journal.
Name: Archiv der Pharmazie
ISSN: 1521-4184
Pages:
Links
- PubMed Source: http://www.ncbi.nlm.nih.gov/pubmed/20806271
- DOI: http://dx.doi.org/10.1002/ardp.200900294
Medical and Biotech [MESH] Definitions
Anti-inflammatory Agents, Non-steroidal
Anti-inflammatory agents that are not steroids. In addition to anti-inflammatory actions, they have analgesic, antipyretic, and platelet-inhibitory actions. They are used primarily in the treatment of chronic arthritic conditions and certain soft tissue disorders associated with pain and inflammation. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. Inhibition of prostaglandin synthesis accounts for their analgesic, antipyretic, and platelet-inhibitory actions; other mechanisms may contribute to their anti-inflammatory effects. Certain NSAIDs also may inhibit lipoxygenase enzymes or TYPE C PHOSPHOLIPASES or may modulate T-cell function. (AMA Drug Evaluations Annual, 1994, p 1814-5)
Mefenamic Acid
A non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory, and antipyretic properties. It is an inhibitor of cyclooxygenase.
Suprofen
An IBUPROFEN-type anti-inflammatory analgesic and antipyretic. It inhibits prostaglandin synthesis and has been proposed as an anti-arthritic.
Salicylates
The salts, esters of salicylic acids, or salicylate esters of an organic acid. Some of these have analgesic, antipyretic, and anti-inflammatory activities by inhibiting prostaglandin synthesis.
Niflumic Acid
An analgesic and anti-inflammatory agent used in the treatment of rheumatoid arthritis.
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