Pafuramidine

Research use only, not for human use.

Pafuramidine (DB289) is an experimental prodrug of the orally active metabolite DB75, a potent antiparasitic compound with anti-malarial activity used in the study of parasitic infections and sleeping sickness.

Pafuramidine (DB289) is an orally active proagent of Furamidine (HY-110137A). Pafuramidine is a potent anti-parasitic agent, can be used to research trypanosomiasis, Pneumocystis pneumonia and malaria.

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Pafuramidine (1-10 mg/kg; p.o.; for 5 or 10 days) cures some trypanosomes-infected monkeys.Pafuramidine (2.5-100 mg/kg; p.o.; for 4 or 5 days) cures some Trypanosoma brucei-infected mice.Animal Model:Vervet monkeys (infected by intravenous injection of 104 trypanosomes) Dosage:1, 3, and 10 mg/kg (group 1/2/3); 10 mg/kg (group 4/5)Administration:p.o.; 5 consecutive days for group 1/2/3 (started on the 7th day postinfection); 10 days for group 4 (started on the 14th day postinfection); 10 days for group 5 (started on the 28th day postinfection). Post-treatment monitoring was maintained for a period of 180 days.Result:Cured all three monkeys in group 3 at 10 mg/kg, and did not recur during the monitoring period.All three monkeys in group 4 became aparasitemic by day 5 of dosing, but only two of three monkeys remained free of blood parasites until 180 days post-treatment monitoring.All three monkeys in group 5 became aparasitemic by day 4 of dosing, but only two of three of monkeys remained free of blood trypanosomes by the end of the 180 days of post-treatment monitoring.Animal Model:Female NMRI mice (infected intraperitoneally with 2 × 104 STIB900 bloodstream forms) Dosage:2.5, 5, 25 and 50 mg/kg Administration:p.o.; for 4 days (started on the 4th day postinfection) Result:Cured all four mice at 25 and 50 mg/kg.Animal Model:Female NMRI mice (infected intraperitoneally with 2 × 104 GVR35 bloodstream forms) Dosage:25, 50 and 100 mg/kg Administration:p.o.; for 5 days (started on the 21st day postinfection) Result:Showed good CNS activity in the GVR35 CNS model, with 3/5 mice cured at 100 mg/kg.

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Microbiology/Virology

Parasite

Parasite | Antibiotic

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186953-56-0

364.4

C20H20N4O3

>98% (HPLC)

In Vitro:?DMSO : 33.33 mg/mL (91.47 mM; Ultrasonic )

N=C(NOC)C=1C=CC(=CC1)C=2OC(=CC2)C=3C=CC(=CC3)C(=N)NOC

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(-20℃)

With Ice Pack

≥ 2 years