Background: NSAIDs have been extensively used for the treatment of pain and inflammation.
There are about 30 different NSAIDs available in market and about 80 percent of prescriptions
throughout the world contains one or the other painkiller. Chronic use of these drugs has many
side effects such as gastric ulceration and the COX-2 inhibitors suffer from major drawback of cardiac
toxicity. The need for a potential and safe NSAIDs has always led to the development of
newer, better and safer drug molecules. In this article design and development of tetrahydrocarbazole
derivatives with very low ulcerative index is reported.
Methods: Fifteen tetrahydrocarbazole derivatives were synthesized on the basis of structural homology
to indomethacin. Compounds were synthesized and characterized on the basis of spectral
data. These were studied for their analgesic, anti-inflammatory and ulcerogenic activities. These
compounds were subjected to molecular docking studies for understanding the possible mechanism
of action and target.
Results: The designed compounds were synthesized successfully in good yield and purity without
much efforts. All compounds were evaluated by in vitro and in vivo assay, molecular modelling
studies and ulcerative index. One of the compound (3-Aminophenyl) (6-chloro-1,2,3,4-tetrahydro-
9H-carbazol-9-yl) methanone 13 was found to be highly active in the in vitro and in vivo assessment
also it was found to be highly safe on ulcerogenic index compared to the standard drugs.
Conclusion: Tetrahydrocarbazoles were found to be promising scaffolds which can be developed
into safe and potential non-steroidal anti-inflammatory agents.