Synthesis, spectral studies and in vitro assessment for antiamoebic activity of new cyclooctadiene ruthenium(II) complexes with 5-nitrothiophene-2-carboxaldehyde thiosemicarbazones.
We report here the synthesis, characterization and in vitro antiamoebic activity of 5-nitrothiophene-2-carboxaldehyde thiosemicarbazones (TSC), 1-5, and their bidentate complexes [Ru(eta(4)-C(8)H(12))(TSC)Cl(2)] 1a-5a. The biological studies of these compounds were investigated against HK-9 strain of Entamoeba histolytica and the concentration causing 50% cell growth inhibition (IC(50)) was calculated in the micromolar range. The ligands exhibited antiamoebic activity in the range (2.05-5.29microM). Screening results indicated that the potencies of the compounds increased by the incorporation of ruthenium(II) in the thiosemicarbazones. The complexes 1a-5a showed antiamoebic activity with an IC(50) of 0.61-1.43microM and were better inhibitors of growth of E. histolytica, based on IC(50) values. The most promising among them is Ru(II) complex 2a having 1,2,3,4-tetrahydroquinoline as N(4) substitution.
Singh
Shailendra
S
Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India.
Athar
Fareeda
F
Azam
Amir
A
D000563:Amebicides / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D004748:Entamoeba histolytica / Q000187:drug effects*; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D012428:Ruthenium; D013329:Structure-Activity Relationship
D000563:Amebicides; D009942:Organometallic Compounds; D012428:Ruthenium