188058-90-4Relevant academic research and scientific papers
Antitrypanosomal, antileishmanial, and antimalarial activities of quaternary arylalkylammonium 2-amino-4-chlorophenyl phenyl sulfides, a new class of trypanothione reductase inhibitor, and of N-acyl derivatives of 2-amino-4-chlorophenyl phenyl sulfide
Parveen, Seheli,Khan, Mohammed O. F.,Austin, Susan E.,Croft, Simon L.,Yardley, Vanessa,Rock, Peter,Douglas, Kenneth T.
, p. 8087 - 8097 (2007/10/03)
Quaternization of the nitrogen atom of 2-amino-4-chlorophenyl phenyl sulfide analogues of chlorpromazine improved inhibition ~40-fold (3′,4′-dichlorobenzyl-[5-chloro-2-phenylsulfanylphenylamino)-propyl] -dimethylammonium chloride inhibited trypanothione r
New spermine and spermidine derivatives as potent inhibitors of trypanosoma cruzi trypanothione reductase
Bonnet, Beatrice,Soullez, David,Davioud-Charvet, Elisabeth,Landry, Valerie,Horvath, Dragos,Sergheraert, Christian
, p. 1249 - 1256 (2007/10/03)
Several spermine and spermidine derivatives containing 2-amino diphenylsulfide substituents were prepared and tested for their inhibiting effects on Trypanosoma cruzi trypanothione reductase. IC50 values were assessed between 0.3 and 3 μM. Compound 32 (K(i) = 0.4 μM) is the most potent TR inhibitor described so far.
New potent inhibitors of trypanothione reductase from Trypanosoma cruzi in the 2-aminodiphenylsulfide series
Girault,Baillet,Horvath,Lucas,Davioud-Charvet,Tartar,Sergheraert
, p. 39 - 52 (2007/10/03)
From a screening assay, 2-aminodiphenylsulfides were selected as leads for trypanothione reductase (TR) inhibition and studied by molecular modelling in the catalytic site of the enzyme. A series of analogues, monomers or bis-derivatives, were synthesized to improve binding energy and therefore inhibiting potency. These compounds appeared to be mixed competitive TR inhibitors and their inhibition profile could be explained when their aggregation in solution was taken into consideration. A bis-aminodiphenylsulfide with an IC50 of 0.55 μM was revealed to be the best TR inhibitor described so far.
