Author
Alia-Cristina Tenchiu
Bio: Alia-Cristina Tenchiu is an academic researcher. The author has contributed to research in topics: Phenylboronic acid & Aryl. The author has an hindex of 4, co-authored 4 publications receiving 80 citations.
Topics: Phenylboronic acid, Aryl, Palladium, Semicarbazone, Ligand
Papers
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TL;DR: A group of 15 aromatic aldehyde 4-(β-d-glucopyranosyl)thiosemicarbazones have been synthesized and evaluated as inhibitors of rabbit muscle glycogen phosphorylase b by kinetic studies, revealing that the inhibitors are accommodated at the catalytic site with the glucopyranusyl moiety at approximately the same position as α- d-glue and stabilize the T conformation of the 280s loop.
31 citations
TL;DR: A series of 22 aromatic aldehyde/ketone 4-(beta-D-glucopyranosyl)thiosemicarbazones have been synthesized by condensation of 4-(per-O-acetylated-beta- D- glucopyrsyl)ThioseMICarbazide with an alde Hyde or a ketone, and then, deacetylation of the resulting product.
26 citations
TL;DR: A palladium-II complex with a known phosphane-free β-d -glucopyranosyl-thiosemicarbazone ligand has been prepared and characterized by spectroscopic studies as mentioned in this paper.
18 citations
TL;DR: A palladium(II) complex with a known inexpensive and very easily synthesized nitrogen-containing bis(phosphinite) ligand has been prepared and characterized by spectroscopic and crystallographic studies.
18 citations
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TL;DR: In this paper, the coordination chemistry of thiosemicarbazone ligands with three (tridentate) or four (tetradentate) potential donor atoms is described.
136 citations
TL;DR: Pincer ligands as mentioned in this paper provide enhanced chemical and thermal stability which serve to minimize the leaching of the metal during the catalytic cycle, and also offer the ability to fine tune the electronic and the steric properties about the metal center, thereby increasing the scope of their applications.
125 citations
TL;DR: Molecular modeling studies results corroborated experimental SAR results, suggesting their use in the design of new antifungal agents, suggesting high selectivity.
90 citations
TL;DR: The design, synthesis, and structure-activity relationships of glucose analogue inhibitors of glycogen phosphorylase were surveyed in this paper, where a number of glucose analogues were presented.
75 citations
TL;DR: The thiosemicarbazones and heterocyclic analogues have been shown to be both antitrypanocidal and inhibitory against parasite cysteine proteases and a series of compounds synthesized and evaluated against cruzain, rhodesain, and SmCB1 through biochemical assays revealed active compounds among this series.
Abstract: 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.
53 citations