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Synthesis of [13 C 6]primaquine

Synthesis of [13C6]primaquine - ResearchGate

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Synthesis of ( 13 C 6 )primaquine - DeepDyve

AB - The effects of chloroquine and primaquine on aminoacylation and polypeptide synthesis in subcellular rat liver systems were investigated. Both drugs exhibited concentration-dependent inhibition of phenylalanine incorporation into aminoacyltRNA. Under conditions where the phenylalanyl-14C-tRNA concentration remained at a "steady state" level, even in the presence of chloroquine or primaquine, the poly U-dependent polyphenylalanine synthesis exhibited concentration-related inhibition by the drugs. When choroquine or primaquine was added several minutes after addition of poly U, the inhibition was not abolished. The drugs did not bring about premature chain termination. Both chloroquine and primaquine inhibited peptidyl transferase, as measured by transfer of polypeptide to puromycin-3H.

Ppt Synthesis-of-primaquine | Powerpoint …

Presentation Summary : It inhibits fungal nucleic acid synthesis. 2. Pharmacokinetics: Well absorbed, used orally ... Primaquine is not effective against the erythrocytic stage of malaria ...

Synthesis of Primaquine and Certain of its Analogs 1

Primaquine phosphate synthesis essay

Formation of primaquine alcohol has also been reported earlier [, ]. The identity of this metabolite was confirmed based on the similarity of its MS/MS fragmentation with the synthetic primaquine alcohol, having the same retention time and UV spectrum. Primaquine alcohol was exclusively generated from the (+)-primaquine enantiomer (Figure B).

The identity of 4-OH-PQ was also confirmed through the synthetic standard with a chromatographic retention time of 2.1 min and m/z 276.25. It was preferentially formed with (−)-primaquine, generating five times the quantity observed with (+)-primaquine. It accounts for about 22% of the total metabolism of (−)-primaquine. The pattern of its generation appears to be complementary to the generation of 2-OH-PQ. It peaked at 30 min in (−)-primaquine with slight drop in the quantity generated over the next 90 min (Figure C).

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Synthesis, characterization, and cellular localization of a fluorescent probe of the antimalarial 8-aminoquinoline primaquine

N2 - The effects of chloroquine and primaquine on aminoacylation and polypeptide synthesis in subcellular rat liver systems were investigated. Both drugs exhibited concentration-dependent inhibition of phenylalanine incorporation into aminoacyltRNA. Under conditions where the phenylalanyl-14C-tRNA concentration remained at a "steady state" level, even in the presence of chloroquine or primaquine, the poly U-dependent polyphenylalanine synthesis exhibited concentration-related inhibition by the drugs. When choroquine or primaquine was added several minutes after addition of poly U, the inhibition was not abolished. The drugs did not bring about premature chain termination. Both chloroquine and primaquine inhibited peptidyl transferase, as measured by transfer of polypeptide to puromycin-3H.

The effects of chloroquine and primaquine on aminoacylation and polypeptide synthesis in subcellular rat liver systems were investigated. Both drugs exhibited concentration-dependent inhibition of phenylalanine incorporation into aminoacyltRNA. Under conditions where the phenylalanyl-14C-tRNA concentration remained at a "steady state" level, even in the presence of chloroquine or primaquine, the poly U-dependent polyphenylalanine synthesis exhibited concentration-related inhibition by the drugs. When choroquine or primaquine was added several minutes after addition of poly U, the inhibition was not abolished. The drugs did not bring about premature chain termination. Both chloroquine and primaquine inhibited peptidyl transferase, as measured by transfer of polypeptide to puromycin-3H.

The effects of chloroquine and primaquine on aminoacylation and polypeptide synthesis in subcellular rat liver systems were investigated
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After suitable calibrations of the substrates and the synthetic metabolites, the initial rate of primaquine (racemate and its enantiomers) metabolism was profiled against the concentration incubated using the SigmaPlot Enzyme Kinetic Software, Module 13.0 (Systat Software Inc, Chicago, IL, USA). The pattern of metabolism was characterized through the Michaelis-Menten plot (N=4; S.D.0.05 in all cases, R2≥0.9) from which the kinetic parameters were determined. Identified metabolites were quantified and profiled against time.

Artesunate (AS) is a medication used to treat malaria

With a retention time of 3.6 min, synthetic 3-OH-PQ was used to confirm the formation of this metabolite with CYP2D6. The level of 3-OH-PQ peaked at 30 min and was formed with 1.5-fold more abundance from (−)-primaquine than with (+)-primaquine, while the levels of 3-OH-PQ generated from (±)-primaquine were apparently the cumulative generation from the individual enantiomers. The 3-OH-PQ also was identified as a stable metabolite (Figure B).

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