Progress in COX-2 inhibitors: a journey so far

Area of Science:

• Pharmacology
• Medicinal Chemistry
• Drug Discovery

Background:

• Non-steroidal anti-inflammatory drugs (NSAIDs) have been used since 1899.
• Traditional NSAIDs inhibit both COX-1 and COX-2, causing gastrointestinal and renal side effects.
• Selective COX-2 inhibitors were developed for improved gastric safety but raised cardiovascular concerns.

Purpose of the Study:

• To review structural classes of selective COX-2 inhibitors developed between 2003-2009.
• To emphasize diaryl-hetero/carbo-cyclic compounds.
• To briefly discuss molecular modeling aspects of these inhibitors.

Main Methods:

• Literature review of selective COX-2 inhibitors.
• Focus on structural diversity and development trends.
• Inclusion of molecular modeling insights.

Main Results:

• Identification of various structural classes of selective COX-2 inhibitors.
• Highlighting diaryl-hetero/carbo-cyclic compounds as a key area.
• Discussion of emerging therapeutic applications beyond inflammation.

Conclusions:

• Selective COX-2 inhibitors present diverse structures and potential applications.
• Cardiovascular risks necessitate careful consideration for the entire NSAID class.
• Further research into selective COX-2 inhibitors for conditions like cancer and neurodegenerative diseases is warranted.