Thiazolyl-N-substituted amides: A group of effective anti-inflammatory agents with potential for local anesthetic properties. Synthesis, biological evaluation, and a QSAR approach
✍ Scribed by Dimitra Hadjipavlou-Litina; Athina Geronikaki; Remi Mgonzo; Irini Doytchinova
- Publisher
- John Wiley and Sons
- Year
- 1999
- Tongue
- English
- Weight
- 177 KB
- Volume
- 48
- Category
- Article
- ISSN
- 0272-4391
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✦ Synopsis
A series of thiazolyl-N-substituted amides were synthesized and tested for anti-inflammatory activity. Their R M values were determined as an expression of their lipophilicity. Theoretical calculation of their lipophilicity, as clog P and log D 7.4 was also performed. The effect of the synthesized compounds on inflammation, using the carrageenan-induced mouse paw edema model was studied. In general, the studied compounds were found to be potent anti-inflammatory agents (23.2-72.1%). Anti-inflammatory activity was influenced by some structural characteristics of the synthesized compounds. An attempt was made to correlate their biological activity with some physicochemical parameters using a quantitative structure-activity relationship approach (QSAR). A parabolic dependence of activity from clog D 7.4 and a linear dependence from surface tension were found. The anti-inflammatory activity of the thiazolyl-amides were found to a great extent to be under pharmacokinetic control.