Pyrazole and its derivatives are an interesting group of heterocyclic compounds as they
exhibit diverse biological activities. Consequently, they have received a great deal of
attention from the scientific community. In this thesis, I have undertaken the synthesis of
four ethyl 1-aryl-5-hydroxy-1H-pyrazole-4-carboxylates, which are inhibitors of
Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH). They were
synthesized according to the procedure described in the literature. The synthesis of the
pyrazole ring was based on the cyclocondensation of the corresponding hydrazine with
diethyl 2-(ethoxymethylene)malonate. Compound 3a was synthesized according to the
one-step procedure described in the literature. Compounds 3b and 3c were obtained by a
slight modification of the literature procedure under basic conditions. Compound 3d was
synthesized using EtOH and Et3N in a ratio of 3:1. All products were characterized by 1H
NMR and IR spectroscopy. The synthesized inhibitors were tested by enzymatic assays
at the Chair of Biochemistry of UL FCCT.
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