European Journal of Medicinal Chemistry p. 104 - 123 (2015)
Update date:2022-08-15
Topics:
Singh, Palwinder
Prasher, Parteek
Dhillon, Parvirti
Bhatti, Rajbir
The indoles bearing a tosyl group at N-1 and a dipeptide substituent at C-3 were screened for anti-inflammatory and anti-hyperalgesic activities. Some of the compounds made significant reduction in the dextran induced swelling and capsaicin induced pain in the albino mice. About 95% reversal in capsaicin induced pain occurred in the presence of 5 mg kg-1of compound 7b, 7d and 7h while diclofenac showed 90% reversal when its 10 mg kg-1 dose was used. In order to examine the mode of action of these compounds; COX-1, COX-2 and 5-LOX enzyme immunoassays were performed. The IC50 of compound 7b for COX-2 and 5-LOX were in the nM range: 5-LOX, IC50 Combining double low line 2.0 nM; COX-2, IC50 Combining double low line 6.3 nM, selectivity for COX-2 over COX-1 was 351. The interactions of the compounds with COX-2 and 5-LOX were supported by the physical parameters including Ki, Ka and δ G. The most potent compounds 7b, 7d and 7h showed no toxicity to the animals and were identified as the promising leads for anti-inflammatory drugs.
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