Abstract
This paper focuses on the synthesis and the in vitro testing of dual COX-1/COX-2 inhibitors. Starting from structures of non-steroidal anti-inflammatory drugs (NSAIDs) the diaryl methanone element was chosen as a lead. Modifications were carried out on this scaffold to obtain potent inhibitors of the COX enzymes. The N-(2-aroylphenyl)sulphonamides and -amides were studied in detail, and to consolidate the data evaluated the corresponding 3- and 4-regioisomers were also investigated. The potency and the enzyme selectivity were varied by structural modifications of the lead.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Animals
-
Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
-
Anti-Inflammatory Agents, Non-Steroidal / chemistry
-
Anti-Inflammatory Agents, Non-Steroidal / pharmacology
-
Blood Platelets / drug effects
-
Blood Platelets / enzymology
-
Cyclooxygenase 1
-
Cyclooxygenase 2
-
Cyclooxygenase 2 Inhibitors
-
Cyclooxygenase Inhibitors / chemical synthesis*
-
Cyclooxygenase Inhibitors / chemistry
-
Cyclooxygenase Inhibitors / pharmacology*
-
Drug Evaluation, Preclinical
-
Isoenzymes / antagonists & inhibitors*
-
Isoenzymes / metabolism
-
Molecular Structure
-
Oxazines / chemistry*
-
Prostaglandin-Endoperoxide Synthases / metabolism
-
Structure-Activity Relationship
Substances
-
Anti-Inflammatory Agents, Non-Steroidal
-
Cyclooxygenase 2 Inhibitors
-
Cyclooxygenase Inhibitors
-
Isoenzymes
-
Oxazines
-
Cyclooxygenase 1
-
Cyclooxygenase 2
-
Prostaglandin-Endoperoxide Synthases