Discovery and optimisation studies of antimalarial phenotypic hits
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.
Mital, Alka,Murugesan, Dinakaran,Kaiser, Marcel,Yeates, Clive,Gilbert, Ian H.
supporting information
p. 530 - 538
(2015/10/12)
SYNTHESIS OF AKALI AND HEAVY METAL DITHIO- AND THIOCARBAMATES BASED ON N-(β-AMINOETHYL)PIPERAZINE
A series of alkali and heavy metal dithio- and thiocarbamates based on N-(β-aminoethyl)piperazine and its derivatives N-(β-piperazinoethyl)imides, N-piperazine, and N-(β-salicylideneaminoethyl)piperazine is prepared.Methods for preparation of dithio- and thiocarbamates based on piperazine are improved.Alkali metal dithio- and thiocarbamates based on piperazines form polymeric complexes with heavy metals.
Zagidullin, R. N.
p. 1275 - 1279
(2007/10/02)
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