Sinefungin and seven analogs were evaluated in vitro for activity against promastigote multiplication of Leishmania donovani, L. tropica, and L. enrietti. Of these compounds, sinefungin, the cyclic derivative, and A9145C were leishmanicidal at concentrations ranging from 0.13 to 2.6 microM. Sinefungin was the most active of these three compounds against L. donovani, and A9145C was most active against L. enrietti. None of the remaining derivatives exhibited significant activity against any one of the three species at the highest dose tested. All agents were assayed for activity against protein methylases I and III. The results of these tests showed that there is no relationship between the inhibition of growth and inhibition of protein methylases I and III.
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Paolantonacci et al. (1985) studied this question.
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