Chemistry:Buparvaquone
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| Formula | C21H26O3 |
| Molar mass | 326.436 g·mol−1 |
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Buparvaquone is a naphthoquinone antiprotozoal drug related to atovaquone. It is a promising compound for the therapy and prophylaxis of all forms of theileriosis. Buparvaquone has been shown to have anti-leishmanial activity in vitro. It can be used to treat bovine East Coast fever protozoa in vitro, along with the only other substance known – Peganum harmala.[citation needed] It is the only really effective commercial therapeutic product against bovine theileriosis, where it has been used since the late 1980s.[citation needed]
Industrial production
It was first produced in Great Britain, then in Germany .[citation needed] Its patent expired in the mid-2000s, and was then produced in different countries, e.g., India and Iran.[citation needed]
Use in bovine theileriosis
Using a single dose of 2,5 mg/kg, the recovery rate of curable cases is 90 to 98%. In tropical theileriosis, a dosage of 2.0 mg/kg has the same efficacy. Body temperature returns to normal in two to five days. Parasitemia lowers from 12% on day 0 to 5% the next day, then to 1% by day 5 and none at day 7.[1]
Molecular target
Buparvaquone resistance appears to be associated with parasite mutations in the Qo quinone-binding site of mitochondrial cytochrome b.[2] Its mode of action is thus likely to be similar to that of the antimalarial drug atovaquone, a similar 2-hydroxy-1,4-naphthoquinone that binds to the Qo site of cytochrome b thus inhibiting Coenzyme Q – cytochrome c reductase.[citation needed]
References
- ↑ "Clinicopathological Studies on Theileria Annulata Infection in Siwa Oasis in Egypt.". BS. Vet. Med. J. 15 (2): 40–6. 2005. http://old.eaap.org/Previous_Annual_Meetings/2005Uppsala/Papers/M2.11_Abdou.pdf.
- ↑ "Point mutations in the Theileria annulata cytochrome b gene is associated with buparvaquone treatment failure". Veterinary Parasitology 187 (3–4): 431–5. July 2012. doi:10.1016/j.vetpar.2012.01.016. PMID 22305656.
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