RESUMO
African sleeping sickness is a potentially fatal neglected disease affecting sub-Saharan Africa. High-throughput screening identified the thiazolyl-benzothiophenamide 1 to be active against the causative parasite, Trypanosoma brucei. This work establishes structure-activity relationships of 1, guiding the design of second generation derivatives. After screening against the clinically relevant species T. b. rhodesiense, the derivative 16 was identified as a suitable candidate for further investigation.
RESUMO
The present investigation is concerned with the synthesis of different acylated 1,2,4-triazole-3-acetates with the objective of discovering novel and potent anti-inflammatory agents. Structures of the synthesized compounds were elucidated by spectral and elemental analyses. The obtained compounds were evaluated for their anti-inflammatory activites as well as gastric ulcerogenic effects and acute toxicity. Results showed that 1-acylated-5-amino-1,2,4-triazole-3-acetates 3a-e showed higher anti-inflammatory activity than the corresponding 5-acylamino derivatives 4a-e in carageenan-induced rat paw edema test with low gastric ulcerogenicity compared with indomethacin. Furthermore, molecular modeling studies were performed in order to rationalize the obtained biological results.
