Synthesis and antiamoebic activity of 3,7-dimethyl-pyrazolo[3,4-e][1,2,4] triazin-4-yl thiosemicarbazide derivatives.
A series of 3,7-dimethyl-pyrazolo[3,4-e][1,2,4]triazin-4-yl thiosemicarbazide derivatives 3-22 were prepared and evaluated in vitro against HM1:1MSS strain of Entamoeba histolytica, to identify the compounds for antiamoebic activity. They exhibited antiamoebic activity in the range (IC50=0.81-7.31microM). The results were compared to the activity of known drug metronidazole. It is inferred from the in vitro studies that the compounds 10, 11, 17 and 18 were found to be significantly better inhibitors of E. histolytica since IC50 values in the muM range elicited by these compounds are much lower than metronidazole. Besides, compounds 11 and 17 have shown the most promising antiamoebic activity (IC50=0.81microM of 11, IC50=0.84 microM of 17 versus IC50=1.81microM of metronidazole). The study suggests the possibility of developing triazine analogues as potential drug candidates for antiamoebic activity.
Singh
Shailendra
S
Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India.
Husain
Kakul
K
Athar
Fareeda
F
Azam
Amir
A
D000563:Amebicides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D004748:Entamoeba histolytica / Q000187:drug effects; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D012663:Semicarbazides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014227:Triazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000563:Amebicides; D012663:Semicarbazides; D014227:Triazines; C005151:thiosemicarbazide