Metal complexes of thiosemicarbazones for imaging and therapy

Review: Pincer ligands—Tunable, versatile and applicable

Synthesis, molecular modeling studies and evaluation of antifungal activity of a novel series of thiazole derivatives

http://chemonet.hu/osztaly/felolvas/fo2012/somsak/crp.pdf

Glucose derived inhibitors of glycogen phosphorylase

The pressing need for better drugs against Chagas disease, African sleeping sickness, and schistosomiasis motivates the search for inhibitors of cruzain, rhodesain, and Schistosoma mansoni CB1 (SmCB1), the major cysteine proteases from Trypanosoma cruzi, Trypanosoma brucei, and S. mansoni, respectively. Thiosemicarbazones and heterocyclic analogues have been shown to be both antitrypanocidal and inhibitory against parasite cysteine proteases. A series of compounds was synthesized and evaluated against cruzain, rhodesain, and SmCB1 through biochemical assays to determine their potency and structure-activity relationships (SAR). This approach led to the discovery of 6 rhodesain, 4 cruzain, and 5 SmCB1 inhibitors with 50% inhibitory concentrations (IC50s) of ≤ 10 μM. Among the compounds tested, the thiosemicarbazone derivative of peracetylated galactoside (compound 4i) was discovered to be a potent rhodesain inhibitor (IC50 = 1.2 ± 1.0 μM). The impact of a range of modifications was determined; removal of thiosemicarbazone or its replacement by semicarbazone resulted in virtually inactive compounds, and modifications in the sugar also diminished potency. Compounds were also evaluated in vitro against the parasites T. cruzi, T. brucei, and S. mansoni, revealing active compounds among this series.

/pdf/synthesis-of-a-sugar-based-thiosemicarbazone-series-and-5e00inbfsn.pdf

Synthesis of a Sugar-Based Thiosemicarbazone Series and Structure-Activity Relationship versus the Parasite Cysteine Proteases Rhodesain, Cruzain, and Schistosoma mansoni Cathepsin B1

The binding of β-D-glucopyranosyl-thiosemicarbazone derivatives to glycogen phosphorylase: A new class of inhibitors

Synthesis and characterization of new aromatic aldehyde/ketone 4-(β-d-glucopyranosyl)thiosemicarbazones

Synthesis of a palladium complex with a β-d-glucopyranosyl-thiosemicarbazone and its application in the Suzuki–Miyaura coupling of aryl bromides with phenylboronic acid

Room-temperature Suzuki–Miyaura coupling of aryl bromides with phenylboronic acid catalyzed by a palladium complex with an inexpensive nitrogen-containing bis(phosphinite) ligand

Alia-Cristina Tenchiu

Papers

The binding of β-D-glucopyranosyl-thiosemicarbazone derivatives to glycogen phosphorylase: A new class of inhibitors

Synthesis and characterization of new aromatic aldehyde/ketone 4-(β-d-glucopyranosyl)thiosemicarbazones

Synthesis of a palladium complex with a β-d-glucopyranosyl-thiosemicarbazone and its application in the Suzuki–Miyaura coupling of aryl bromides with phenylboronic acid

Room-temperature Suzuki–Miyaura coupling of aryl bromides with phenylboronic acid catalyzed by a palladium complex with an inexpensive nitrogen-containing bis(phosphinite) ligand