1H-Pyrido[3,4-b]indole-3-carboxylic acid, 1-(2,4-dichlorophenyl)-2,3,4,9-tetrahydro-, (1R,3S)-

Uses

MMV008138 is a species-selective IspD (enzyme 2-C-methyl-d-erythritol 4-phosphate cytidylyltransferase)-targeting antimalarial agent, with an IC50 of 44 nM for PfIspD (P. falciparum IspD). MMV008138 inhibits the growth of P. falciparum Dd2 strain with an IC50 of 250 nM[1][2].

IC 50

Plasmodium

References

[1] Ghavami M, et al. Biological Studies and Target Engagement of the 2- C-Methyl-d-Erythritol 4-Phosphate Cytidylyltransferase (IspD)-Targeting Antimalarial Agent (1 R,3 S)-MMV008138 and Analogs. ACS Infect Dis. 2018 Apr 13;4(4):549-559. DOI:10.1021/acsinfecdis.7b00159
[2] Yao ZK, et al. Determination of the active stereoisomer of the MEP pathway-targeting antimalarial agent MMV008138, and initial structure-activity studies. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1515-9. DOI:10.1016/j.bmcl.2015.02.020