Abstrakt

Synthesis And Antiinflamation Activity Of Bis(Diacetylmonoxime) Thiocarbohydrazone And Its Cu(II) Complex

Ahmed A.El-Asmy, Gamil A.Al-Hazmi, Yousery E.Sherif, Sami A.Gabr

Some thiosemicarbazone derivatives have been prepared, characterized and predicted through quantitative structure activity relationship (QSAR) to show their inhibition of cyclooxygenase-2-enzyme(COX-2). Bis(diacetylmonoxime) thicarbohydrazone[H3DMT] was found more analgesic and ulceroggenic. The descriptors are mainly derived from molecular orbital calculations by the semiemperical AM1 method. The inhibition activity was found to depend on polarizability of the molecule. The study herein is focused on testing the inflammatory activity of Cu(II) acetate, H3DMT and [Cu2(HDMT)2(H2O)] using collagen–adjuvant arthritis model in rats. The observed anti-inflammatory of H3DMT and [Cu2(HDMT)2(H2O)] makes an importance for future profiting due to their ability to COX-2 inhibition and the high metal legibility.