Decoquinate 

Decoquinate is an orally active, selective inhibitor of the mitochondrial bc1 complex, targeting Eimeria spp. sporozoites and first generation schizonts, and Plasmodium spp. Decoquinate inhibits electron transfer by competitively binding to the mitochondrial cytochrome b system, blocking the parasite's energy metabolism, thereby inhibiting its development and reproduction. Decoquinate has significant anticoccidial activity, preventing intestinal damage and improving host growth performance, and also has inhibitory effects on the liver and blood stages of Plasmodium. Decoquinate is mainly used in veterinary research to prevent and treat coccidiosis in ruminants and poultry^[1][2][3].

1. In vitro antimalarial experiment: Decoquinate (nanoformulation; 48-72 h) significantly inhibited the growth of Plasmodium falciparum in the liver and blood stages in vitro, with an IC₅₀ of 2.18 ng/mL for the liver stage and 0.05 ng/ml for the blood stage.[2] 2. Derivative activity experiment: Decoquinate derivatives had a strong inhibitory effect on Chloroquine (HY-17589A) sensitive strain NF54 and resistant strains K1 and W2, with an activity 5 times that of Decoquinate, and low toxicity to human fibroblasts.[3]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1. Coccidiosis prevention and treatment experiment:
Decoquinate (0.5-1 mg/kg; administered in feed; once daily; for at least 28 days) effectively inhibits and prevents coccidiosis in the coccidiosis model of ruminants (calves, lambs, goats), reduces intestinal damage and oocyst excretion, and improves host growth performance. Decoquinate effectively treats and prevents coccidiosis, reduces intestinal damage and oocyst excretion, and improves host growth performance^[1].
2. Toxoplasma prevention experiment:
Decoquinate (2 mg/kg; administered in feed; once daily; for 14 weeks) can prevent abortion and perinatal loss caused by Toxoplasma infection in pregnant sheep Toxoplasma infection model, delay febrile reaction and reduce placental damage^[1].
3. Antimalarial experiment of nanoformulation:
Decoquinate nanoformulation (1.25 mg/kg; oral; once a day; 3 days) significantly inhibits the growth of liver-stage Plasmodium in a mouse Plasmodium infection model, with an efficacy 15 times that of microparticle formulation^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

417.54

C₂₄H₃₅NO₅

18507-89-6

Solid

White to off-white

O=C(C1=C(O)C2=CC(OCCCCCCCCCC)=C(OCC)C=C2N=C1)OCC

Room temperature in continental US; may vary elsewhere.

• [1]. Taylor MA, et, al. The history of decoquinate in the control of coccidial infections in ruminants. J Vet Pharmacol Ther. 2012 Oct;35(5):417-27.  [Content Brief]

  [2]. Wang H, et al. Nanoparticle formulations of decoquinate increase antimalarial efficacy against liver stage Plasmodium infections in mice. Nanomedicine. 2014 Jan;10(1):57-65.  [Content Brief]

  [3]. Beteck RM, et al. Straightforward conversion of decoquinate into inexpensive tractable new derivatives with significant antimalarial activities. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3006-3009.  [Content Brief]