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30652-11-0

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30652-11-0 Usage

Description

Deferiprone, the first oral iron chelator, was marketed in India for the management of thalassaemia. Patients with thalassaemia, a blood related genetic disorder, require life time transfusion which causes excessive deposition of iron in liver and spleen, subsequent damage to organs and eventually death unless iron is removed by a chelator. Deferiprone is a potent iron chelator that mobilizes excessive iron from iron storage proteins ferritin and hemosiderin, from iron saturated transferrin and lactoferrin, but not from hemoglobin. The deferiprone-iron complex is excreted in urine and bile. Deferiprone was reportedly well accepted by patients and no hematological toxicity was observed. Deferiprone has also been demonstrated as an effective and safe chelator in the mobilization of aluminum.

Chemical Properties

White Needles

Originator

Cipla (India)

Uses

Different sources of media describe the Uses of 30652-11-0 differently. You can refer to the following data:
1. 3-Hydroxy-1,2-dimethyl-4(1H)-pyridone (OH-pyridone) may be used in the bacterial killing assays. It has been employed as hydroxyketone chelating agent and its cytotoxic action against oral human normal and tumor cell lines has been evaluated.
2. iron chelating agent
3. A chelator that could replace disferrioxamine. It is orally and parenterally effective in the removal of iron in vivo from rabbits and mice and also from transferrin and ferritin in vitro

Definition

ChEBI: A member of the class of 4-pyridones that is pyridin-4(1H)-one substituted at positions 1 and 2 by methyl groups and at position 3 by a hydroxy group. A lipid-soluble iron-chelator used for treatment of thalassaemia.

Brand name

Kelfer

General Description

3-Hydroxy-1,2-dimethyl-4(1H)-pyridone (Hdpp, Deferiprone) is a hydroxy ketone derivative. It reacts with uranyl salts [UO2(NO3)2] in aqueous acidic solution to afford mono nuclear complexes ([UO2(dpp)(Hdpp)2(H2O)]ClO4). X-ray studies have been conducted to examine the structure and geometry of these complexes.

Clinical Use

Orally administered chelator:Treatment of transfusional iron overload

Drug interactions

Potentially hazardous interactions with other drugsNone known.

Metabolism

Deferiprone is hepatically metabolised to an inactive glucuronide metabolite and is excreted mainly in the urine as the metabolite and the iron-deferiprone complex, with a small amount of unchanged drug.

References

1) Hider and Hoffbrand (2018),?The Role of Deferiprone in Iron Chelation; N. Engl. J. Med.,?379?2140 2) Sripetchwandee?et al.?(2016),?A combination of an iron chelator with an antioxidant effectively diminishes the dendritic loss, tau-hyperphosphorylation, amyloid-β accumulation and brain mitochondrial dynamic disruption in rats with chronic iron-overload., Neuroscience?332?191 3) Liu?et al.?(2018),?Iron and Alzheimer’s Disease: From Pathogenesis to Therapeutic Implications;?Front. Neurosci,?12?632

Check Digit Verification of cas no

The CAS Registry Mumber 30652-11-0 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 3,0,6,5 and 2 respectively; the second part has 2 digits, 1 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 30652-11:
(7*3)+(6*0)+(5*6)+(4*5)+(3*2)+(2*1)+(1*1)=80
80 % 10 = 0
So 30652-11-0 is a valid CAS Registry Number.
InChI:InChI=1/C7H9NO2/c1-5-6(9)3-4-8(2)7(5)10/h3-4,10H,1-2H3

30652-11-0 Well-known Company Product Price

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  • Aldrich

  • (379409)  3-Hydroxy-1,2-dimethyl-4(1H)-pyridone  98%

  • 30652-11-0

  • 379409-5G

  • 723.06CNY

  • Detail
  • Aldrich

  • (379409)  3-Hydroxy-1,2-dimethyl-4(1H)-pyridone  98%

  • 30652-11-0

  • 379409-25G

  • 2,620.80CNY

  • Detail

30652-11-0SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 11, 2017

Revision Date: Aug 11, 2017

1.Identification

1.1 GHS Product identifier

Product name deferiprone

1.2 Other means of identification

Product number -
Other names CP20

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:30652-11-0 SDS

30652-11-0Synthetic route

1,2-dimethyl-3-(benzyloxy)-4(1H)-pyridinone
90037-22-2

1,2-dimethyl-3-(benzyloxy)-4(1H)-pyridinone

deferiprone
30652-11-0

deferiprone

Conditions
ConditionsYield
With hydrogen; palladium on activated charcoal In methanol for 2h;80%
With hydrogen; palladium on activated charcoal In tetrahydrofuran under ambient conditions;65%
With concentrated hydrobromic acid
Maltol
118-71-8

Maltol

methylamine
74-89-5

methylamine

deferiprone
30652-11-0

deferiprone

Conditions
ConditionsYield
In water for 10h; Reflux;69%
In water at 160 - 162℃; under 6750.5 Torr; for 0.0216667h; Irradiation;65%
In water for 6.5h; Heating;60%
isomaltol
3420-59-5

isomaltol

methylamine
74-89-5

methylamine

deferiprone
30652-11-0

deferiprone

Conditions
ConditionsYield
In water for 20h; Heating;64%
3-(β-D-galactopyranosyloxy)-2-furanyl methyl ketone
82756-28-3

3-(β-D-galactopyranosyloxy)-2-furanyl methyl ketone

methylamine
74-89-5

methylamine

deferiprone
30652-11-0

deferiprone

Conditions
ConditionsYield
In water for 20h; Heating;49%
Maltol
118-71-8

Maltol

methylamine hydrochloride
593-51-1

methylamine hydrochloride

deferiprone
30652-11-0

deferiprone

Conditions
ConditionsYield
With potassium hydroxide In water at 50℃;25%
deferiprone
30652-11-0

deferiprone

[(hydrotris(3,5-phenylmethylpyrazolyl)borato)CoCl]

[(hydrotris(3,5-phenylmethylpyrazolyl)borato)CoCl]

[(hydrotris(3,5-phenylmethylpyrazolyl)borato)Co(3,4-HOPO)]

[(hydrotris(3,5-phenylmethylpyrazolyl)borato)Co(3,4-HOPO)]

Conditions
ConditionsYield
With (C2H5)3N In methanol; dichloromethane (C2H5)3N added to a soln. of Co complex, a soln. of ligand in MeOH added, stirred at room temp. overnight under N2; evapd. (vac.), dissolved in C6H6, filtered, crystd. by diffusion of the soln. with pentane; elem. anal.;98%
deferiprone
30652-11-0

deferiprone

bismuth (III) nitrate pentahydrate

bismuth (III) nitrate pentahydrate

terephthalic acid
100-21-0

terephthalic acid

water
7732-18-5

water

N,N-dimethyl-formamide
68-12-2, 33513-42-7

N,N-dimethyl-formamide

[Bi2(1,4-benzenedicarboxylate)(deferiprone-H)4(H2O)2]·2DMF

[Bi2(1,4-benzenedicarboxylate)(deferiprone-H)4(H2O)2]·2DMF

Conditions
ConditionsYield
at 100℃; for 72h; Sealed tube; High pressure;98%
deferiprone
30652-11-0

deferiprone

water
7732-18-5

water

tantalum pentaethoxide
150747-55-0

tantalum pentaethoxide

tris(1,2-dimethyl-3-hydroxy-4(1H)-pyridone)oxotantalum

tris(1,2-dimethyl-3-hydroxy-4(1H)-pyridone)oxotantalum

Conditions
ConditionsYield
In methanol; water addn. of soln. of tantalum compd. in methanol to soln. of deferiprone inmethanol, stirring at room temp. overnight, addn. of water, stirring fo r 30 min; evapn. at 40°C, washing with warm CHCl3, filtration, drying in vac., elem. anal.;97%
dichloro(mesitylene)ruthenium(II) dimer

dichloro(mesitylene)ruthenium(II) dimer

deferiprone
30652-11-0

deferiprone

[RuCl(C7H8NO2)(C6H3(CH3)3)]
176792-83-9

[RuCl(C7H8NO2)(C6H3(CH3)3)]

Conditions
ConditionsYield
With NaOCH3 In methanol; water byproducts: NaCl; (N2); reflux (3 h); solvent removal, dissoln. (CH2Cl2), filtration (Celite), evapn.; elem. anal.;93%
deferiprone
30652-11-0

deferiprone

methyl trifluoromethanesulfonate
333-27-7

methyl trifluoromethanesulfonate

Trifluoro-methanesulfonate3-hydroxy-4-methoxy-1,2-dimethyl-pyridinium;

Trifluoro-methanesulfonate3-hydroxy-4-methoxy-1,2-dimethyl-pyridinium;

Conditions
ConditionsYield
In chloroform for 3h; Heating;90%
dichloro(pentamethylcyclopentadienyl)rhodium (III) dimer

dichloro(pentamethylcyclopentadienyl)rhodium (III) dimer

deferiprone
30652-11-0

deferiprone

sodium methylate
124-41-4

sodium methylate

Rh(C5(CH3)5)Cl(C5H2NO2(CH3)2)
173413-67-7

Rh(C5(CH3)5)Cl(C5H2NO2(CH3)2)

Conditions
ConditionsYield
In methanol byproducts: NaCl; N2-atmosphere; stoich. amts., refluxing for 3 h; solvent removal, extn. into CH2Cl2, filtration (Celite), evapn., recrystn. (CH2Cl2/Et2O);90%
deferiprone
30652-11-0

deferiprone

zinc(II) chloride
7646-85-7

zinc(II) chloride

bis-(3-hydroxy-1,2-dimethyl-4-pyridinonato)zinc(II)

bis-(3-hydroxy-1,2-dimethyl-4-pyridinonato)zinc(II)

Conditions
ConditionsYield
With NaOH In methanol; water raising of the pH to 7 with dilute NaOH, concn.,; cooling, filtration, elem. anal.;90%
deferiprone
30652-11-0

deferiprone

2,5-dihydroxybenzoic acid.
490-79-9

2,5-dihydroxybenzoic acid.

C7H6O4*C7H9NO2

C7H6O4*C7H9NO2

Conditions
ConditionsYield
In ethanol; acetone at 60℃; for 2h;90%
In ethanol; acetone at 20 - 45℃; for 73.7h; Sealed tube;36.5 mg
deferiprone
30652-11-0

deferiprone

4-hydroxy-benzoic acid
99-96-7

4-hydroxy-benzoic acid

C7H6O3*C7H9NO2

C7H6O3*C7H9NO2

Conditions
ConditionsYield
In water at 60℃; for 2h;90%
deferiprone
30652-11-0

deferiprone

vanadyl
20644-97-7

vanadyl

bis(1,2-dimethyl-3-hydroxy-4-pyridinonato)oxidovanadium(IV)

bis(1,2-dimethyl-3-hydroxy-4-pyridinonato)oxidovanadium(IV)

Conditions
ConditionsYield
With NaOH In water under Ar; ligand suspended in water; heated at 50-60°C; VO(2+) soln. and solid NaOH added; chilled; filtered; solid washed with water and acetone; dried in vac.; elem. anal.;86%
deferiprone
30652-11-0

deferiprone

p-toluenesulfonyl chloride
98-59-9

p-toluenesulfonyl chloride

1,2-dimethyl-4-oxo-1,4-dihydropyridin-3-yl 4-methylbenzenesulfonate
1259401-68-7

1,2-dimethyl-4-oxo-1,4-dihydropyridin-3-yl 4-methylbenzenesulfonate

Conditions
ConditionsYield
With pyridine at 20℃; Inert atmosphere;86%
dichloro(pentamethylcyclopentadienyl)rhodium (III) dimer

dichloro(pentamethylcyclopentadienyl)rhodium (III) dimer

deferiprone
30652-11-0

deferiprone

Rh(C5(CH3)5)Cl(C5H2NO2(CH3)2)
173413-67-7

Rh(C5(CH3)5)Cl(C5H2NO2(CH3)2)

Conditions
ConditionsYield
85%
deferiprone
30652-11-0

deferiprone

[ruthenium(II)(η6-1-methyl-4-isopropyl-benzene)(chloride)(μ-chloride)]2
52462-29-0

[ruthenium(II)(η6-1-methyl-4-isopropyl-benzene)(chloride)(μ-chloride)]2

[(p-cymene)Ru(C7H8NO2)Cl]
252573-94-7

[(p-cymene)Ru(C7H8NO2)Cl]

Conditions
ConditionsYield
With NaOMe In methanol; dichloromethane addn. of 1 equiv. NaOMe (in MeOH) to ligand (in CH2Cl2), addn. to stoich. amt. of metal complex (in CH2Cl2), standing for 2 h; solvent removal (vac.), extn. into Et2O/CH2Cl2=1:2, evapn. (reduced pressur), drying (vac.); elem. anal.;85%
chloro(1,5-cyclooctadiene)iridium(I) dimer

chloro(1,5-cyclooctadiene)iridium(I) dimer

deferiprone
30652-11-0

deferiprone

[Ir(C8H12)(CH3NCHCHCOCOC(CH3))]*0.5H2O

[Ir(C8H12)(CH3NCHCHCOCOC(CH3))]*0.5H2O

Conditions
ConditionsYield
With MeONa In methanol; dichloromethane inert atm.; 4 h; evapn. (vac.), extraction (Et2O/CH2Cl2 1:2), evapn., drying (vac.); elem. anal.;85%
deferiprone
30652-11-0

deferiprone

manganese (II) acetate tetrahydrate
6156-78-1

manganese (II) acetate tetrahydrate

Mn(1,2-dimethyl-3-hydroxy-4-pyridinone(1-))3*2.5H2O

Mn(1,2-dimethyl-3-hydroxy-4-pyridinone(1-))3*2.5H2O

Conditions
ConditionsYield
With sodium acetate trihydrate In methanol to soln. ligand and AcONa*3H2O in MeOH Mn(OAc)2*4H2O was added and refluxed for 4 h; react. mixt. was cooled to room temp., ppt. was filtered, washed with Et2O and dried in vacuo overnight; elem. anal.;84.6%
deferiprone
30652-11-0

deferiprone

chromium chloride hexahydrate

chromium chloride hexahydrate

fac-Cr(III)(3-oxy-2-methyl-4-pyridinone)3*2H2O

fac-Cr(III)(3-oxy-2-methyl-4-pyridinone)3*2H2O

Conditions
ConditionsYield
With triethylamine In methanol CrCl3*6H2O added to soln. of deferiprone and triethylamine in CH3OH, mixt. refluxed for 4 h, cooled to room temp.; solid filtered off, washed with cold methanol and ether, dried under vac., recrystd. from water; elem. anal.;84.4%
deferiprone
30652-11-0

deferiprone

vanadyl sulfate *3.6H2O

vanadyl sulfate *3.6H2O

bis(1,4-dihydro-1,2-dimethyl-4-oxo-3-pyridinolato)oxovanadium (IV)
186321-59-5, 175662-51-8

bis(1,4-dihydro-1,2-dimethyl-4-oxo-3-pyridinolato)oxovanadium (IV)

Conditions
ConditionsYield
With potassium hydroxide In water to a soln. of 1-hydroxy-4,6-dimethyl-2(1H)-pyrimidinone in water added dropwise a soln. of VOSO4*3.6H2O in water, pH of the soln. adjusted to 10with 2M KOH, stirred overnight; precipitate collected by filtration, washed several times with H2O, dried over anhydrous P2O5 in vacuo, elem. anal.;84%
deferiprone
30652-11-0

deferiprone

manganese(ll) chloride

manganese(ll) chloride

Mn(1,2-dimethyl-3-hydroxy-4-pyridinone(1-))2Cl*0.25H2O

Mn(1,2-dimethyl-3-hydroxy-4-pyridinone(1-))2Cl*0.25H2O

Conditions
ConditionsYield
With triethylamine In acetonitrile to soln. ligand and Et3N in MeCN MnCl2 was added and refluxed for 6 h; react. mixt. was cooled to room temp. and concd. in vacuo, cold Et2O wasadded, ppt. was filtered, washed with Et2O and dried in vacuo overnight ; elem. anal.;83.8%
methanol
67-56-1

methanol

deferiprone
30652-11-0

deferiprone

1,2-dimethyl-2-methoxy-1,2-dihydro-pyridine-3,4-dione

1,2-dimethyl-2-methoxy-1,2-dihydro-pyridine-3,4-dione

Conditions
ConditionsYield
With silver(l) oxide at 45℃; for 2h;83%
vanadyl sulfate trihydrate

vanadyl sulfate trihydrate

deferiprone
30652-11-0

deferiprone

bis(1,2-dimethyl-3-hydroxy-4-pyridinonato)oxidovanadium(IV)

bis(1,2-dimethyl-3-hydroxy-4-pyridinonato)oxidovanadium(IV)

Conditions
ConditionsYield
With KOH In water under aerobic conditions; VOSO4*3H2O in hot water added slowly to suspn.of ligand (molar ratio 1:2) in hot water; aq. soln. of KOH (2 equiv.) a dded (pH ca. 3); refluxed for 2 h; ppt. collected; washed with acetone; dried overnight in vac.; satisfactory elem. anal.;83%
deferiprone
30652-11-0

deferiprone

tetracarbonyldi-μ-chlorodirhodium(I)

tetracarbonyldi-μ-chlorodirhodium(I)

[Rh(CO)2(CH3NCHCHCOCOC(CH3))]
250638-50-7

[Rh(CO)2(CH3NCHCHCOCOC(CH3))]

Conditions
ConditionsYield
With MeONa In methanol; dichloromethane 4 h; evapn. (vac.), extraction (Et2O/CH2Cl2 1:2), evapn., drying (vac.); elem. anal.;83%
deferiprone
30652-11-0

deferiprone

di-μ-chlorobis{2-[(dimethylamino)methyl]phenyl-C,N}dipalladium (II)

di-μ-chlorobis{2-[(dimethylamino)methyl]phenyl-C,N}dipalladium (II)

[Pd(CH3NCHCHCOCOC(CH3))((CH3)2NCH2C6H4)]
250717-07-8, 250638-60-9

[Pd(CH3NCHCHCOCOC(CH3))((CH3)2NCH2C6H4)]

Conditions
ConditionsYield
With NaOMe In methanol; dichloromethane 2 h; evapn. (vac.), extraction (Et2O/CH2Cl2), evapn., drying (vac., 50°C); elem. anal.;83%
deferiprone
30652-11-0

deferiprone

water
7732-18-5

water

manganese(ll) chloride

manganese(ll) chloride

Mn(1,2-dimethyl-3-hydroxy-4-pyridinone(1-))2(H2O)2*0.5H2O

Mn(1,2-dimethyl-3-hydroxy-4-pyridinone(1-))2(H2O)2*0.5H2O

Conditions
ConditionsYield
With triethylamine In acetonitrile under N2 atm. to slurry MnCl2 in MeCN was added soln. ligand and Et3N inMeCN, mixt. was refluxed for overnight; soln. was cooled to room temp., volume was reduced by stream N2 gas, cold Et2O was added, solid was filtered, washed with MeCN, Et2O, dried under vac. overnight; elem. anal.;83%
deferiprone
30652-11-0

deferiprone

zinc(II) nitrate hexahydrate

zinc(II) nitrate hexahydrate

terephthalic acid
100-21-0

terephthalic acid

water
7732-18-5

water

3Zn(2+)*2C8H4O4(2-)*2C7H8NO2(1-)*2H2O

3Zn(2+)*2C8H4O4(2-)*2C7H8NO2(1-)*2H2O

Conditions
ConditionsYield
In ethanol at 95℃; for 24h;82%
methanol
67-56-1

methanol

beryllium(II) sulphate tetrahydrate

beryllium(II) sulphate tetrahydrate

deferiprone
30652-11-0

deferiprone

Be(dpp)2*MeOH
449141-30-4

Be(dpp)2*MeOH

Conditions
ConditionsYield
With NH3 In water 3-hydroxy-1,2-dimethyl-4-pyridinone was added to BeSO4*4H2O in water, after dissolution pH was adjusted to 8.5 with concd. NH3; solvent was evapd. at 323-333 K and cooled to room temp., ppt. was filtered off, washed with cold water, and dried in air, recrystn. from MeOH/Et2O; elem. anal.;81%
deferiprone
30652-11-0

deferiprone

dichlorobis(triethylphosphine)-μ-dichlorodipalladium(II)

dichlorobis(triethylphosphine)-μ-dichlorodipalladium(II)

[PdCl(CH3NCHCHCOCOC(CH3))(P(C2H5)3)]*0.5H2O

[PdCl(CH3NCHCHCOCOC(CH3))(P(C2H5)3)]*0.5H2O

Conditions
ConditionsYield
With NaOMe In methanol; dichloromethane 2 h; evapn. (vac.), extraction (Et2O/CH2Cl2), evapn., drying (vac., 50°C); elem. anal.;80%
deferiprone
30652-11-0

deferiprone

uranyl nirate hexahydrate

uranyl nirate hexahydrate

sodium perchlorate

sodium perchlorate

[UO2(3-oxy-1,2-dimethyl-4(1H)-pyridone)2(H2O)]

[UO2(3-oxy-1,2-dimethyl-4(1H)-pyridone)2(H2O)]

Conditions
ConditionsYield
In water slow evapn. of aq. soln. of 0.1 M NaClO4, pyridone-compound, uranyl-compound at room temp. at pH 3; elem. anal.;80%
deferiprone
30652-11-0

deferiprone

trans-di-μ-chloro-bis[chloro(tributylphosphine)palladium]

trans-di-μ-chloro-bis[chloro(tributylphosphine)palladium]

[PdCl(CH3NCHCHCOCOC(CH3))(P(C4H9)3)]
250638-59-6

[PdCl(CH3NCHCHCOCOC(CH3))(P(C4H9)3)]

Conditions
ConditionsYield
With NaOMe In methanol; dichloromethane inert atm.; 2 h; evapn. (vac.), extraction (Et2O/CH2Cl2), evapn., drying (vac., 50°C); elem. anal.;78%
deferiprone
30652-11-0

deferiprone

zinc(II) nitrate hexahydrate

zinc(II) nitrate hexahydrate

terephthalic acid
100-21-0

terephthalic acid

N,N-dimethyl-formamide
68-12-2, 33513-42-7

N,N-dimethyl-formamide

3Zn(2+)*2C8H4O4(2-)*2C7H8NO2(1-)*2C3H7NO

3Zn(2+)*2C8H4O4(2-)*2C7H8NO2(1-)*2C3H7NO

Conditions
ConditionsYield
at 100℃; for 24h;77%

30652-11-0Relevant articles and documents

Dissociation of CP20 from iron(II)(cp20)3: A pulse radiolysis study

Merkofer, Martin,Domazou, Anastasia,Nauser, Thomas,Koppenol, Willem H.

, p. 671 - 675 (2006)

Deferiprone (CP20), a hydroxypyridine-4-one, is used in iron-chelation therapy. For the iron(III)-/(II)(cp20)3 couple, a standard electrode potential of -620 mV was measured by cyclic voltammetry [Templeton et al., Inorg. Chim. Acta 1996, 245, 199; Merkofer et al., Helv. Chim. Acta 2004, 87, 3021]. On the basis of this value and the overall stability constant for the equilibrium of iron(III) and three CP20 molecules, ligand dissociation ought to take place after reduction of the iron(III)(cp20)3 complex. By pulse radiolysis, we show that hydrated electrons reduce the iron(III)(cp20) 3 complex with a rate constant of k = (6.4 ± 0.3) × 1010 M-1S-1, and that the iron(II)(cp20) 3 complex aquates rapidly. The dissociation of the first two CP20 molecules takes place within a few μs after the pulse. The dissociation rate constant for the last CP20 ligand is (8 ± 1) × 103 S-1. The observation of a dissociation illustrates that, under dilute conditions, iron(II) is not fully complexed by CP20 and could potentially participate in redox cycling to produce oxyradicals. The CO2 - radical does not reduce iron(III)(cp20)3, which indicates that this complex reacts, as expected, very slowly with inner-sphere reductants. Wiley-VCH Verlag GmbH & Co. KGaA, 2006).

Interaction between the low molecular mass components of blood serum and the VO(IV)-DHP system (DHP = 1,2-dimethyl-3-hydroxy-4(1H)-pyridinone)

Buglyo, Peter,Kiss, Tamas,Kiss, Erzsebet,Sanna, Daniele,Garribba, Eugenio,Micera, Giovanni

, p. 2275 - 2282 (2002)

In order to estimate the impact of the low molecular mass (l.m.m.) VO(IV) binders of blood serum on the potentially insulin-enhancing drug [VO(DHP)2] [DHP = 1,2-dimethyl-3-hydroxy-4(1H)-pyridinone], the speciation in the binary system VO(IV)-DHP and in the ternary systems VO-DHP-ligand B (B = oxalate, lactate, citrate or phosphate) was studied by pH-potentiometry at 25.0°C and at an ionic strength I = 0.2 mol dm-3 (KCl). The binding modes of the complexes formed were determined by spectroscopic (electronic absorption and EPR) techniques. DHP was found to form stable mono and bis complexes via the coordination of (O,O) chelate(s). Through displacement of the oxo group of VO(IV), the tris complex is also formed, especially at a high excess of ligand. The results in the ternary systems demonstrate that, at physiological pH, none of the B ligands can compete with DHP; [VO(DHP)2] therefore seems to remain almost completely intact, even in the presence of citrate, the strongest competitor among these B ligands. These findings indicate that, for DHP, unlike maltol or picolinic acid, ternary complex formation and thus transformation reactions with the l.m.m. binders of biofluids, is almost negligible. From among the three carrier molecules, only DHP can effeciently compete with serum transferrin for binding of VO(IV).

Synthesis, Modification, and Biological Evaluation of a Library of Novel Water-Soluble Thiopyridone-Based Organometallic Complexes and Their Unexpected (Biological) Behavior

Gajic, Natalie,Happl, Barbara,Harringer, Sophia,Hejl, Michaela,Jakupec, Michael A.,Kandioller, Wolfgang,Kast, Caroline,Keppler, Bernhard K.,Koellensperger, Gunda,Legin, Anton A.,Ozenil, Marius,Roller, Alexander,Schweikert, Andreas,Wernitznig, Debora

, (2020/04/20)

A series of 16 dinuclear thiopyridone-based organometallics with excellent water solubility, increased stability and remarkable cytotoxicity were synthesized and characterized. The complexes of this work formed dimeric species featuring a double positive charge in polar protic solvents, accounting for their outstanding solubility in aqueous solution. Most of them displayed higher antiproliferative activity than their parental thiomaltol complex, with unexpected cytotoxicity trends depending on the employed metal center, ligand modification, and cell line. Insights into their behavior in biological systems were gathered by means of amino-acid interaction studies, cytotoxicity tests in 3D spheroid models, laser ablation, cellular accumulation measurements, as well as cell cycle experiments.

Application of 1-aryl-4-pyridone compound

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Paragraph 0071-0074, (2020/01/12)

The invention discloses application of a 1-aryl-4-pyridone compound, and provides application of a compound of a structure of a formula (I) shown in the description in inhibiting activity of plant pathogenic bacteria. The compound of the structure of the formula (I) shown in the description has outstanding broad-spectrum antifungal activity upon plant pathogenic bacteria in agricultural production, and meanwhile, has a prevention and treatment effect on bacterial disease of crops. In-vivo biological assay shows that the compound of the structure of the formula (I) shown in the description hasa prevention and control effect greater than 95% on cucumber downy mildew, cucumber target leaf spot, wheat scab and tomato gray mold. Meanwhile, results of postharvest fresh-keeping tests of mangos show that the compound is capable of effectively controlling postharvest diseases of mangos and in addition, prolonging the fresh-keeping time of the mangos. In addition, results show that the compoundis also capable of effectively controlling bacterial leaf blight of rice in pot experiments, and is more effective than a commercial fungicide zhongshengmycin. In conclusion, the 1-aryl-4-pyridone derivative of the formula (I) shown in the description has broad-spectrum plant pathogenic fungus resistance and bacterial activity, and is a type of lead compounds with wide bioactivity.

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