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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2016/06/15 19:40:34」(JST)
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Sulfalene
|
Systematic (IUPAC) name |
4-Amino-N-(3-methoxypyrazinyl)benzenesulfonamide
|
Clinical data |
Trade names |
Eadazine, Kelfizina, Kelfizine W, Longum |
Drugs.com |
International Drug Names |
Routes of
administration |
Oral[1] |
Pharmacokinetic data |
Protein binding |
60 to 80%[1] |
Biological half-life |
60 to 65 hours[1] |
Excretion |
Urinary[1] |
Identifiers |
CAS Number |
152-47-6 Y |
ATC code |
J01ED02 (WHO) QJ01EQ19 (WHO) |
PubChem |
CID 9047 |
DrugBank |
DB00664 Y |
ChemSpider |
8695 Y |
UNII |
T6BL4ZC15G Y |
KEGG |
D01216 Y |
Synonyms |
Sulfametopyrazine |
Chemical data |
Formula |
C11H12N4O3S |
Molar mass |
280.304 g/mol |
SMILES
-
O=S(=O)(Nc1nccnc1OC)c2ccc(N)cc2
|
InChI
-
InChI=1S/C11H12N4O3S/c1-18-11-10(13-6-7-14-11)15-19(16,17)9-4-2-8(12)3-5-9/h2-7H,12H2,1H3,(H,13,15) Y
-
Key:KXRZBTAEDBELFD-UHFFFAOYSA-N Y
|
(verify) |
Sulfalene (INN, USAN) or sulfametopyrazine (BAN) is a long-acting sulfonamide antibacterial used for the treatment of chronic bronchitis, urinary tract infections and malaria.[2][3] As of 2014 there were only two countries in which it is currently still marketed: Thailand and Ireland.[3]
It was discovered by researchers at Farmitalia and first published in 1960 and was marketed as Kelfizina.[4][5]
See also
References
- ^ a b c d "Sulfalene". MIMS Drug Information System. Retrieved 26 August 2011.
- ^ DrugBank DB00664
- ^ a b Brayfield, A, ed. (9 May 2013). "Sulfametopyrazine". Martindale: The Complete Drug Reference. Pharmaceutical Press. Retrieved 28 March 2014.
- ^ Baruffa G. Clinical trials in Plasmodium falciparum malaria with a long-acting sulphonamide. Trans R Soc Trop Med Hyg. 1966;60(2):222-4. PMID 5332105
- ^ Per prior citation, the first publication: Camerino B, Palamidessi G (1960) Derivati della parazina II. Sulfonamdopir (in Italian). Gazz Chim Ital 90:1802–1815
Antibacterials: nucleic acid inhibitors (J01E, J01M)
|
|
Antifolates
(inhibits
purine metabolism,
thereby inhibiting
DNA and RNA synthesis) |
DHFR inhibitor |
- 2,4-Diaminopyrimidine
- Trimethoprim#
- Brodimoprim
- Tetroxoprim
- Iclaprim†
|
|
Sulfonamides
(DHPS inhibitor) |
Short-
acting |
- Sulfaisodimidine
- Sulfamethizole
- Sulfadimidine
- Sulfapyridine
- Sulfafurazole
- Sulfanilamide
- Sulfathiazole
- Sulfathiourea
|
|
Intermediate-
acting |
- Sulfamethoxazole
- Sulfadiazine#
- Sulfamoxole
|
|
Long-
acting |
- Sulfadimethoxine
- Sulfadoxine
- Sulfalene
- Sulfametomidine
- Sulfametoxydiazine
- Sulfamethoxypyridazine
- Sulfaperin
- Sulfamerazine
- Sulfaphenazole
- Sulfamazone
|
|
Other/ungrouped |
- Sulfacetamide
- Sulfadicramide
- Sulfametrole
|
|
|
Combinations |
- Trimethoprim/sulfamethoxazole#
|
|
|
Topoisomerase
inhibitors/
quinolones/
(inhibits
DNA replication) |
1st g. |
- Cinoxacin‡
- Flumequine‡
- Nalidixic acid‡
- Oxolinic acid‡
- Pipemidic acid‡
- Piromidic acid‡
- Rosoxacin‡
|
|
Fluoro-
quinolones |
2nd g. |
- Ciprofloxacin#
- Ofloxacin
- Enoxacin‡
- Fleroxacin‡
- Lomefloxacin‡
- Nadifloxacin‡
- Norfloxacin‡
- Pefloxacin‡
- Rufloxacin‡
|
|
3rd g. |
- Levofloxacin
- Balofloxacin‡
- Grepafloxacin‡
- Pazufloxacin‡
- Sparfloxacin‡
- Temafloxacin‡
- Tosufloxacin‡
|
|
4th g. |
- Besifloxacin
- Gatifloxacin
- Finafloxacin
- Gemifloxacin
- Moxifloxacin
- Clinafloxacin†
- Garenoxacin‡
- Prulifloxacin‡
- Sitafloxacin‡
- Trovafloxacin‡/Alatrofloxacin‡
|
|
Vet. |
- Danofloxacin
- Difloxacin
- Enrofloxacin
- Ibafloxacin
- Marbofloxacin
- Orbifloxacin
- Pradofloxacin
- Sarafloxacin
|
|
|
Newer non-fluorinated |
|
|
Related (DG) |
- Aminocoumarins: Novobiocin
|
|
|
Anaerobic DNA
inhibitors |
Nitro- imidazole derivatives |
- Metronidazole#
- Tinidazole
- Ornidazole
|
|
Nitrofuran derivatives |
- Nitrofurantoin#
- Furazolidone‡
- Nifurtoinol
|
|
|
RNA synthesis |
Rifamycins/
RNA polymerase |
- Rifampicin#
- Rifabutin
- Rifapentine
- Rifaximin
- Rifalazil§
|
|
|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
|
|
English Journal
- Nitrogen-14 nuclear quadrupole resonance spectroscopy: a promising analytical methodology for medicines authentication and counterfeit antimalarial analysis.
- Barras J1, Murnane D, Althoefer K, Assi S, Rowe MD, Poplett IJ, Kyriakidou G, Smith JA.
- Analytical chemistry.Anal Chem.2013 Mar 5;85(5):2746-53. doi: 10.1021/ac303267v. Epub 2013 Feb 20.
- We report the detection and analysis of a suspected counterfeit sample of the antimalarial medicine Metakelfin through developing nitrogen-14 nuclear quadrupole resonance ((14)N NQR) spectroscopy at a quantitative level. The sensitivity of quadrupolar parameters to the solid-state chemical environme
- PMID 23384229
- Identification of isobaric amino-sulfonamides without prior separation.
- Barry SJ1, Wolff JC.
- Rapid communications in mass spectrometry : RCM.Rapid Commun Mass Spectrom.2012 Feb 29;26(4):419-29. doi: 10.1002/rcm.6118.
- RATIONALE: Direct analysis mass spectrometry (DAMS) techniques offer increased speed of analysis without the need for sample preparation or prior separation. A feature of these techniques is that all ionisable species will typically be analysed at the same time which makes the ability to distinguish
- PMID 22279018
- Design and synthesis of new N-(5-trifluoromethyl)-1H-1,2,4-triazol-3-yl benzenesulfonamides as possible antimalarial prototypes.
- Boechat N1, Pinheiro LC, Santos-Filho OA, Silva IC.
- Molecules (Basel, Switzerland).Molecules.2011 Sep 20;16(9):8083-97. doi: 10.3390/molecules16098083.
- A rational approach was used to synthesize a new set of 15 1H-1,2,4-triazol-3-yl benzenesulfonamide derivatives with the aim of developing new antimalarial lead compounds. These derivatives were prepared in yields between 50% and 62%, and their structures were elucidated using IR, ¹H-, ¹³C-, ¹�
- PMID 21934646
Japanese Journal
- 実験的トキソプラズマ症の治療に関する基礎的研究:(II) マウスの急性および慢性トキソプラズマ症心筋内虫体に及ばすAcetylspiramycinとSulfa剤あるいは牛血清由来免疫賦活物質 (CSP-II) の併用効果
- 慢性薬剤起因性肝内胆汁うっ滞症の1剖検例:肝内胆管系に関する形態学的研究
- 薬剤投与によるトキソプラズマRH株およびBeverley株の毒性を変える試み
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- Sulfamethopyrazine(Policydal)の眼科的応用 大石 正夫 [他] この論文をさがす NDL-OPAC CiNii Books 収録刊行物 眼科臨床医報 眼科臨床医報 63(6), 482-485, 1969-06 眼科臨床医 ...
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