63500-82-3Relevant articles and documents
SO2F2-Mediated N-Alkylation of Imino-Thiazolidinones
Bernier, David,Donnard, Morgan,Jeschke, Peter,Leroux, Frédéric R.,Panossian, Armen,Pazenok, Sergii,Santos, Laura,Vors, Jean-Pierre
, (2021)
The N-alkylation of ambident and weakly nucleophilic imino-thiazolidinones has been developed via substitution with alkyl fluorosulfonates. These reactive electrophiles are obtained through the transformation of nontoxic, economic, and commercially availa
Discovery and optimisation studies of antimalarial phenotypic hits
Mital, Alka,Murugesan, Dinakaran,Kaiser, Marcel,Yeates, Clive,Gilbert, Ian H.
supporting information, p. 530 - 538 (2015/10/12)
There is an urgent need for the development of new antimalarial compounds. As a result of a phenotypic screen, several compounds with potent activity against the parasite Plasmodium falciparum were identified. Characterization of these compounds is discussed, along with approaches to optimise the physicochemical properties. The in vitro antimalarial activity of these compounds against P. falciparum K1 had EC50 values in the range of 0.09e29 mM, and generally good selectivity (typically >100-fold) compared to a mammalian cell line (L6). One example showed no significant activity against a rodent model of malaria, and more work is needed to optimise these compounds.
REACTIVITY AND TAUTOMERISM OF AZOLIDINES. XLIII. KINETICS OF THE METHYLATION OF 2-PHENYLIMINO-4-THIAZOLIDINONE SODIUM SALT WITH DIMETHYL SULFATE IN ACETONITRILE
Basova, Yu. G.,Ramsh, S. M.,Ginak, A. I.
, p. 1940 - 1944 (2007/10/02)
The kinetics of the methylation of 2-phenylimino-4-thiazolidinone sodium salt with dimethyl sulfate in acetonitrile were studied at 5, 15, and 25 deg C.In acetonitrile the sodium salt exists as an equilibrium mixture of free ions and intimate ion pairs.The reaction rate constants of the free ions were determined by means of Acree's equation.The intimate ion pairs are practically nonreactive particles.The thermodynamic activation parameters were determined from the temperature dependence of the methylation rate constants of the free ions.