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Síntese, avaliação biológica de alguns 2,3-di-hidropirazóis e tiazóis como agentes anti-inflamatórios e antibacterianos

  Abdel-Sattar S. Hamad Elgazwy, Ekhlass Nassar and Myssoune Y. Zaki

The present article describes the synthesis of two novel series of 5-(benzofuran-2-yl)-3-(4-(piperidin-1-yl)phenyl)- 2,3-dihydropyrazole-1-carbothioamide 6 and 1-(4-(3-(benzofuran-2-yl)-2-(4-arylthiazol-2-yl)-2,5-dihydro-1H-pyrazol- 5-yl)phenyl)piperidine 8a-d. All the newly synthesized target compounds (3, 4, 5, 6 and 8a-d) were screened for their in vivo anti-inflammatory (AI) activity using carrageenan-induced rat paw edema assay and in vitro antibacterial activity against two Gram-positive and two Gram-negative bacteria. All eight compounds (3, 4, 5, 6, and 8a-d) showed consistently excellent AI activity (≥ 70% inhibition), at 3 and 4 h after the carrageenan injection, comparable to that of standard drug indomethacin (78%) whereas the remaining twelve compounds have shown significant activity with 57–75% inhibition after 3 h and 56–63% inhibition after 4 h. All the tested compounds showed moderate antibacterial properties.