pteridine reductase-1 (ptr1)

TbPTR1 inhibitor 2 is identified as a new development of improved pteridine reductase-1 (PTR1) inhibitors and anti-trypanosomatidic agents[1].

Insecticidal agent 19 (Compound 7b) exhibits antimalarial activity by inhibiting dihydrofolate reductase-thymidylate synthase (DHFR-TS) and pteridine reductase 1 (PTR1) through the folate metabolic pathway. This compound also inhibits the promastigote and amastigote forms of Leishmania major, with IC50 values of 1.43 μM and 3.78 μM, respectively.

CYP3A4-IN-5 (Compound 5p) is a potent inhibitor of Leishmania major pteridine reductase 1 (Lm PTR1), with an IC50 value of 12.77 µM. This compound holds potential for research in parasitic infections.

TbPTR1 inhibitor 1 (compound 5d) is an effective inhibitor of kinetochore pteridine reductase 1 (PTR1). The IC50 of TbPTR1 inhibitor 1 against Trypanosoma brucei PTR1 (TbPTR1) is <0.1 nM, and its EC50 against Trypanosoma brucei is 0.66 μM.

Antileishmanial agent-21 (compound 4e) functions as an inhibitor of Leishmania pteridine reductase 1 (Lm-PTR1), employing an anti-folate mechanism. Its antileishmanial effects can be negated by folic acid and leucovorin. Additionally, it demonstrates inhibitory activity against the chloroquine-resistant Plasmodium falciparum strain RKL9, with an IC50 ranging from 0.0198 to 0.096 μM [1].