Pyronaridine
Pyronaridine Basic information
- Product Name:
- Pyronaridine
- Synonyms:
-
- 4-[(7-CHLORO-2-METHOXY-1,5-DIHYDROBENZO[B][1,5]NAPHTHYRIDIN-10-YL)IMINO]-2,6-BIS(PYRROLIDIN-1-YLMETHYL)CYCLOHEXA-2,5-DIEN-1-ONE
- Malaridine phosphate
- 4-(7-chloro-2-Methoxybenzo[b][1,5]naphthyridin-10-ylaMino)-2,6-bis(pyrrolidin-1-ylMethyl)phenol
- Pyronaridine
- 4-(2-Methoxy-6-chloro-1,10-diazaanthracene-9-ylamino)-2,6-bis(pyrrolizinomethyl)phenol
- 4-[(7-Chloro-2-methoxybenzo[b]-1,5-naphthyridin-10-yl)amino]-2,6-bis(1-pyrrolidinylmethyl)phenol
- Phenol, 4-[(7-chloro-2-methoxybenzo[b]-1,5-naphthyridin-10-yl)amino]-2,6-bis(1-pyrrolidinylmethyl)-
- 4-[(7-chloro-2-methoxy-1,5-dihydrobenzo[b][1,5]naphthyridin-...
- CAS:
- 74847-35-1
- MF:
- C29H32ClN5O2
- MW:
- 518.05
- EINECS:
- 1533716-785-6
- Product Categories:
-
- john's
- Mol File:
- 74847-35-1.mol
Pyronaridine Chemical Properties
- Boiling point:
- 621.3±55.0 °C(Predicted)
- Density
- 1.356±0.06 g/cm3 (20℃ 760 Torr)
- refractive index
- 1.5650 (estimate)
- solubility
- DMSO (Slightly), Water (Slightly)
- form
- Solid
- pka
- 8.20±0.50(Predicted)
- color
- Light Yellow to Orange
- Stability:
- Incompatible with strong oxidizing agents.
- CAS DataBase Reference
- 74847-35-1
Pyronaridine Usage And Synthesis
Chemical Properties
solid
Definition
ChEBI: Pyronaridine is an aminoquinoline.
Antimicrobial activity
Pyronaridine is active against the asexual erythrocytic stage of P. falciparum with little or no activity against gametocytes or the hepatic stage. In-vitro blood schizonticide activities are in the range of 0.001–0.03 mg/L, showing a moderate correlation to chloroquine resistance. However, this correlation varies between studies and does not seem to be clinically significant. It is also active against P. vivax, P. ovale and P. malariae. Antagonistic interactions with artemisinins were reported in vitro, but synergy with artesunate has been observed in rodent models.
Acquired resistance
Decreasing in-vitro sensitivity has been observed in China.
Pharmaceutical Applications
An aza-aminoacridine formulated for oral use. A Mannichbase derivative of mepacrine.
Pharmacokinetics
Peak plasma concentrations are reached after 3–14 h depending upon the formulation; there is also considerable interindividual variation. Elimination half-lives of 63–190 h have been reported, again dependent upon the formulation.
Clinical Use
Treatment of uncomplicated P. falciparum and P. vivax malaria
A fixed-dose combination with artesunate (Pyramax) is being
developed for uncomplicated P. falciparum and P. vivax malaria.
Side effects
It is well tolerated and no outstanding toxic effects have been reported.
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Pyronaridine(74847-35-1)Related Product Information
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- 1,5-NAPHTHYRIDINE
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- 1,5-NAPHTHYRIDIN-4-AMINE
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- Pyranoridine phosphate
- N-DESETHYL AMODIAQUINE
- 3-(PYRROLIDIN-1-YLMETHYL)ANILINE
- M6407
- [3-(1-PYRROLIDINYLMETHYL)PHENYL]METHANAMINE
- 1-{3-[(METHYLAMINO)METHYL]BENZYL}PYRROLIDINE 90+%N-METHYL-3-(PYRROLIDIN-1-YLMETHYL)BENZYLAMINE
- 7-CHLORO-10-(4-HYDROXYANILINO)-2-METHOXY BENZO(B)-1,5-NAPHTHY RIDINE
- Pyronaridine
- Amopyroquine