4085-31-8 Usage
Description
Piperaquine phosphate is an aminoquinoline compound characterized by its chemical structure, which features 1,3-di(piperazin-1-yl)propane with the nitrogen at position 4 of each of the piperazine moieties replaced by a 7-chloroquinolin-4-yl group. It is a white crystalline powder known for its pharmaceutical applications.
Uses
Used in Pharmaceutical Industry:
Piperaquine phosphate is used as an antimalarial drug for treating malaria caused by Plasmodium parasites. It is particularly effective against drug-resistant strains of the parasite, making it a valuable component in the fight against malaria.
Used in Drug Delivery Systems:
In the field of drug delivery, Piperaquine phosphate is utilized as a component in the development of novel drug delivery systems. These systems aim to improve the bioavailability, efficacy, and targeted delivery of the compound, enhancing its therapeutic potential in treating various diseases, including malaria.
Used in Research and Development:
Piperaquine phosphate is also used as a research compound in the development of new pharmaceuticals and drug candidates. Its unique chemical properties and known antimalarial activity make it an interesting starting point for the design and synthesis of new drugs with improved properties and broader applications.
Biological Activity
piperaquine, an antimalarial drug, is first synthesised in the 1960s and extensively used as prophylaxis and treatment during the next 20 years.
in vitro
in 280 p. falciparum isolates, the ic50 for piperaquine ranged from 9.8 nm to 217.3 nm and a significant but low correlation was observed between the ic50 values for piperaquine and chloroquine. however, the coefficient of determination indicated that only 2.1% of the variation in the response to piperaquine was explained by the variation in the response to chloroquine. moreover, the mean value for piperaquine was 74.0 nm in the pfcrt k76 wild-type group and 87.7 nm in the 76t mutant group and such difference was not significant [1].
in vivo
male sd rats were orally administered piperaquine or as a short-term i.v. infusion. results showed that piperaquine disposition was best described by a 3-compartment model with a rapid initial distribution phase after i.v. administration. the pk of piperaquine was characterized by a low clearance, a large volume of distribution and a long terminal half-life [2].
IC 50
9.8 to 217.3 nm for p. falciparum isolates
references
[1] pascual a et al. in vitro piperaquine susceptibility is not associated with the plasmodium falciparum chloroquine resistance transporter gene. malar j. 2013 nov 25;12:431. [2] tarning j, lindegardh n, sandberg s, day nj, white nj, ashton m. pharmacokinetics and metabolism of the antimalarial piperaquine after intravenous and oral single doses to the rat. j pharm sci. 2008 aug;97(8):3400-10.[3] denis mb, davis tm, hewitt s, incardona s, nimol k, fandeur t, poravuth y, lim c, socheat d. efficacy and safety of dihydroartemisinin-piperaquine (artekin) in cambodian children and adults with uncomplicated falciparum malaria. clin infect dis. 2002 dec 15;35(12):1469-76.
Check Digit Verification of cas no
The CAS Registry Mumber 4085-31-8 includes 7 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 4 digits, 4,0,8 and 5 respectively; the second part has 2 digits, 3 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 4085-31:
(6*4)+(5*0)+(4*8)+(3*5)+(2*3)+(1*1)=78
78 % 10 = 8
So 4085-31-8 is a valid CAS Registry Number.
4085-31-8Relevant articles and documents
AN IMPROVED PROCESS FOR THE PREPARATION OF PIPERAQUINE
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, (2011/09/14)
The present invention relates to an improved process for the preparation of 7-chloro- 4-piperazin-1-yl-quinoline of formula (I), a key intermediate for the synthesis of Piperaquine or its pharmaceutically acceptable salts.