Medicinal chemistry

1. Anti-inflammatory Agents
-Shashank Shekhar Mishra

2. NSAIDs

3. Features of Inflammation

7. Nonsteroidal Anti-inflammatory drugs
Mechanism of Action-

8.  NSAIDs inhibit cycloxygenase (COX), the enzyme that catalyses the
synthesis of cyclic endoperoxides, from the arachidonic acid to form PGs. The
two COX isoenzymes are COX-1 and COX-2.
 The function of COX-1 is to produce PGs that are involved in normal cellular
activity, (protection of gastric mucosa, maintenance of kidney function). While,
COX-2 is responsible for the production of PGs at the inflammation sites. Most
NSAIDs inhibit both COX-1 and COX-2 with varying degree of selectivity.
Selective COX-2 inhibitor may eliminate the side effects associated with
NSAIDs due to COX-1 inhibition, such as gastric and renal effect.

9. Classification of NSAIDs
A. Nonselective COX inhibitors
1. Salicylic acid derivatives:
- Aspirin
- Sodium salicylate

10. 2. p-Amino phenol derivatives:
- Paracetamol
- Phenacetin

11. 3. Pyrazolidinedione derivatives:
- Phenyl butazone
4. Oxicams:
- Piroxicam

12. 5. Anthranilic acid derivatives:
- Mefenemic acid - Meclofenamate
6. Aryl alkanoic acid derivative -
a. Indole acetic acid: b. Indene acetic acid:
- Indomethacin - Sulindac

13. c. Pyrrole acetic acid:
- Tolmetin -Zomepirac
d. Phenyl acetic (propionic) acid:
-Ibuprofen -Naproxen

14. - Diclofenac - Ketorolac
7. Pyrazolones:
- Phenazone (Antipyrine)

15. B. Selective COX-2 inhibitors

16. Synthesis of Mefenamic acid

17. Synthesis of Ibuprofen

18. Thank You