Synthesis and biological activity of new potential antimalarial: 1H-pyrazolo[3,4-b]pyridine derivatives

The appearance of drug resistant Plasmodium falciparum malaria necessitates the search for novel antimalarial agents. Using the classical ring-bioisosterism concept as a strategy to develop new potential drugs, 1H-pyrazolo[3,4-b]pyridine 4-aminomethanol compounds were designed and synthesized as iso...

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Bibliographic Details
Published in:	Bollettino chimico farmaceutico Vol. 139; no. 1; p. 14
Main Authors:	Dias, L R, Freitas, A C, Barreiro, E J, Goins, D K, Nanayakkara, D, McChesney, J D, Dias, R S
Format:	Journal Article
Language:	English
Published:	Italy 01-01-2000
Subjects:	Animals Antimalarials - chemical synthesis Antimalarials - pharmacology Antimalarials - toxicity Cercopithecus aethiops Chloroquine - pharmacology Plasmodium falciparum - drug effects Pyridines - chemical synthesis Pyridines - pharmacology Pyridines - toxicity Vero Cells
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Summary:	The appearance of drug resistant Plasmodium falciparum malaria necessitates the search for novel antimalarial agents. Using the classical ring-bioisosterism concept as a strategy to develop new potential drugs, 1H-pyrazolo[3,4-b]pyridine 4-aminomethanol compounds were designed and synthesized as isosteres of the classical quinoline antimalarial mefloquine. The hydrochloride form of these compounds were tested for in vitro antimalarial activity against chloroquine-sensitive (Sierra Leone D-6) and resistant (Indochina W-2) clones of P. falciparum. The results described herein indicated that 1-H-pyrazolo[3,4-b]pyridine system represents a bioisosteric framework to quinoline system in the antimalarial activity.
ISSN:	0006-6648