Synthesis and gametocidal activity of 1-aryl-5-(aminocarbonyl)-1H-pyrazole-4-carboxylic acids
1992
Lynch, M.P. | Ackmann, S.A. | Heim, D.R. | Davis, G.E. | Staszak, M.A. | Beck, J.R. | Tschabold, E.E. | Wright, F.L.
A series of 1-aryl-5-(aminocarbonyl)-1H-pyrazole-4-carboxylic acids were serendipitously discovered to be chemical hybridizing agents. Different synthetic routes were developed for the active analogs depending on whether an electron withdrawing group or electron donating group was present on the phenyl ring. Development of the "second generation gametocides" produced analogs which were 5-6 times more active than the original lead.
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