Your browser doesn't support javascript.
loading
Show: 20 | 50 | 100
Results 1 - 1 de 1
Filter
Add more filters










Database
Type of study
Language
Publication year range
1.
Arzneimittelforschung ; 52(6): 482-8, 2002.
Article in English | MEDLINE | ID: mdl-12109050

ABSTRACT

The development of new antimalarial drugs is an urgent priority considering the increasing prevalence of drug-resistant Plasmodium falciparum parasites. A series of pyrazoles are described as part of efforts directed toward the synthesis of some potent antimalarial agents. The replacement of the ester group as a substituent in the pyrazole ring by nitrile group caused a precipitous loss of activity as antimalarial due to the lack of hydrogen-bond formation. Further modification of the heterocyclic ring to give substituted aryl derivatives afforded potent antimalarial derivatives: methyl 5-amino-3-anisidinepyrazole-4-carboxylic acid 3a (IC50: 0.149 mumol/l) and methyl 5-amino-3-(m anisidin)pyrazole-4-carboxylic acid 3c (IC50: 0.15 mumol/l). The synthesis, structure-activity relationships (SAR), X-ray crystallography and pharmacological activity associated with these series of compounds are discussed.


Subject(s)
Antimalarials/chemical synthesis , Antimalarials/pharmacology , Plasmodium falciparum/drug effects , Pyrazoles/chemical synthesis , Pyrazoles/pharmacology , Animals , Antimalarials/chemistry , Crystallography, X-Ray , Erythrocytes/parasitology , Hydrogen Bonding , Indicators and Reagents , Magnetic Resonance Spectroscopy , Models, Molecular , Pyrazoles/chemistry , Spectrophotometry, Infrared , Structure-Activity Relationship
SELECTION OF CITATIONS
SEARCH DETAIL
...