5416-00-2Relevant academic research and scientific papers
Catalyst- and organic solvent-free synthesis of thioacids in water
Elagawany, Mohamed,Hegazy, Lamees,Elgendy
supporting information, p. 2018 - 2021 (2019/07/03)
Thioacids and thioamino acids were synthesized in excellent yields from readily available acyl benzotriazoles and sodium hydrosulfide in water at room temperature. The new methodology features mild reaction conditions, high yields, short reaction times, and does not involve the use of organic solvents or bases. The reaction is eco-friendly, and the workup procedure is simple and does not require chromatographic separation.
Anti-leishmanial activity of novel homo- and heteroleptic bismuth(iii) thiocarboxylates
Andrews, Philip C.,Junk, Peter C.,Kedzierski, Lukasz,Peiris, Roshani M.
, p. 1297 - 1305 (2013/10/22)
Two new thiocarboxylic acids, p-bromothiobenzoic BTA and thionaphthoic acid TNA, and five new homo- and heteroleptic bismuth(iii) compounds derived from thiocarboxylic acids: [Bi{S(C≤O)C6H4Br}3] 1, [PhBi{S(C≤O)C6H4Br}2] 2, [Bi{S(C≤O)C10H7}3] 3, [PhBi{S(C≤O)C10H7}2] 4, and [Ph2Bi{S(C≤O)C10H7}] 5 were synthesised and fully characterised. The solid-state structure of complex [PhBi{S(C≤O)C6H4Br}2] 2 was confirmed by X-ray crystallography. In complex 2, the two thiocarboxylate ligands are coordinated to the bismuth(iii) centre in a didentate fashion, forming a distorted octahedral geometry in which the phenyl group and the lone pair are oriented axial to the plane formed by the two thiocarboxylate ligands. Long-range Bi-S interactions (3.54A) link these monomeric units to form a one-dimensional polymer. These compounds, in addition to six previously synthesised complexes: [Bi{SC(≤O)C6H5}3] 6, [PhBi{SC(≤O)C6H5}2] 7, [Ph2Bi{SC(≤O)C6H5}] 8, [Bi{SC(≤O)C6H4NO2}3] 9, [PhBi{SC(≤O)C6H4NO2}2] 10, and [PhBi{SC(≤O)C6H4SO3}] 11, and the thiocarboxylic acids themselves, were assessed for their in vitro activity against Leishmania major promastigotes, and for general toxicity against human fibroblast cells. The thiocarboxylic acids, with the exception of thiobenzoic acid and sulfothiobenzoic acid, were toxic to both L. major parasites and the mammalian cells at high concentrations of 50-100M. The bismuth(iii) thiocarboxylate derivatives proved to be more active than the corresponding acids. Among these, the heteroleptic phenyl-substituted bismuth(iii) complexes 2, 4, 5, and 7 were highly active, showing IC50 (half maximal inhibitory concentration) values ranging from 0.39 to 4.69M, and a clear ligand dependence on activity.
ACYLSULFONAMIDES AND PROCESSES FOR PRODUCING THE SAME
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Page/Page column 103; 104, (2012/03/09)
The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.
