2015
DOI: 10.1007/s00775-015-1239-5
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Synthesis, characterization and urease inhibition, in vitro anticancer and antileishmanial studies of Ni(II) complexes with N,N,N′-trisubstituted thioureas

Abstract: A series of N,N,N'-trisubstituted thioureas (1-12) and their Ni(II) complexes (1a-12a) were synthesized and characterized by multinuclear ((1)H and (13)C) NMR, FT-IR spectroscopy and LC-MS techniques in combination with elemental analysis. The crystal structures of both ligands and Ni(II) chelates of type Ni(L-O, S)2 were determined by single crystal X-ray diffraction analysis. All the complexes were adopted to have square planar geometry, where the N,N,N'-trisubstituted thioureas showed bidentate mode of coor… Show more

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Cited by 51 publications
(27 citation statements)
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“…Urease inhibition activity of the synthesized compounds was determined by the indophenol method [26] with small modifications [27]. Reaction mixtures comprised of 40 μL of buffer (100 mM urea, 0.01 M K 2 HPO 4 , 1 mM EDTA and 0.01 M LiCl 2 , pH 8.2) and 10 μL of jack-bean urease enzyme (5 U/mL) were incubated with 10 μL of P. domestica gum solution and the nanoparticles (1 mg/mL) at 37 °C for 30 min in 96-well plates.…”
Section: Methodsmentioning
confidence: 99%
“…Urease inhibition activity of the synthesized compounds was determined by the indophenol method [26] with small modifications [27]. Reaction mixtures comprised of 40 μL of buffer (100 mM urea, 0.01 M K 2 HPO 4 , 1 mM EDTA and 0.01 M LiCl 2 , pH 8.2) and 10 μL of jack-bean urease enzyme (5 U/mL) were incubated with 10 μL of P. domestica gum solution and the nanoparticles (1 mg/mL) at 37 °C for 30 min in 96-well plates.…”
Section: Methodsmentioning
confidence: 99%
“…Urea moiety is commonly found in various potent leishmanicidal compounds (17,18). On the other hand, the thiourea scaffold has been described for treating parasitic disorders by itself (19,20) or combined with metals (21). Finally, we further expanded the scope of the reaction to the synthesis of selenoureas in order to assess the importance of the number of selenium atoms in the leishmanicidal activity.…”
mentioning
confidence: 99%
“…Thus, this spacer causes a drop in the leishmancidal activity in selenoureas, while in ureas and thioreas it is responsible for a significant increase. With regard to the introduction of alkyl side chains, this modification confers a marked leishmanicidal increase in the three series of compounds (9,10,11,20,21,22,46, 47, and 48), with seven of them being more active than miltefosine. This phenomenon indicates that the activity correlates with an increase in the lipophilicity of the compounds.…”
mentioning
confidence: 99%
“…All the complexes show a high frequency shift in the H and C resonances for the carboxylate ligands relative to those observed in the NMR spectra of the free acids. In addition, the NMR spectra of the antimony(V) complexes show resonances for the aromatic protons in the expected range of 6.86–8.23 ppm …”
Section: Resultsmentioning
confidence: 99%