Details
Stereochemistry | ACHIRAL |
Molecular Formula | C11H12N4O3S |
Molecular Weight | 280.303 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=C(NS(=O)(=O)C2=CC=C(N)C=C2)N=CC=N1
InChI
InChIKey=KXRZBTAEDBELFD-UHFFFAOYSA-N
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)
DescriptionSources: https://www.drugbank.ca/drugs/DB00664Curator's Comment: description was created based on several sources, including
https://www.drugs.com/international/sulfalene.html | https://www.ncbi.nlm.nih.gov/pubmed/137981 | https://www.ncbi.nlm.nih.gov/pubmed/4888027 | https://www.ncbi.nlm.nih.gov/pubmed/5864358
Sources: https://www.drugbank.ca/drugs/DB00664
Curator's Comment: description was created based on several sources, including
https://www.drugs.com/international/sulfalene.html | https://www.ncbi.nlm.nih.gov/pubmed/137981 | https://www.ncbi.nlm.nih.gov/pubmed/4888027 | https://www.ncbi.nlm.nih.gov/pubmed/5864358
Sulfalene (INN, USAN) or Sulfametopyrazine (BAN) is a long-acting sulfonamide antibiotic used for the treatment of chronic bronchitis, urinary tract infections, and malaria. Sulfametopyrazine, by virtue of a long half-life, achieves peak blood levels of 120 mkg/ml or more which fall to around 30-50 mkg/ml one week after a single oral dose of 2 g. Long-term administration of this drug in the treatment of leprosy for up to 3 years has been accomplished without serious unwanted effects
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL2364668 Sources: https://www.ncbi.nlm.nih.gov/pubmed/25775967 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Sources: https://www.ncbi.nlm.nih.gov/pubmed/4888027 |
Curative | Kelfizina Approved UseUnknown |
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Primary | Sulfametopyrazine Approved UseUnknown |
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Primary | Kelfizina Approved UseUnknown |
PubMed
Title | Date | PubMed |
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Hypoxia and oxidative stress. Tumour hypoxia--therapeutic considerations. | 2001 |
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Specific growth rate of bifidobacteria cultured on different sugars. | 2002 |
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Potential antiamoebic property of the roots of Piper longum Linn. | 2002 Nov |
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Evolution of mosaic operons by horizontal gene transfer and gene displacement in situ. | 2003 |
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Viability of microencapsulated bifidobacteria in simulated gastric juice and bile solution. | 2003 Sep 15 |
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Anti-inflammatory activities of Aller-7, a novel polyherbal formulation for allergic rhinitis. | 2004 |
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Comparative genomics of gene-family size in closely related bacteria. | 2004 |
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Pharmacokinetic and pharmacodynamic studies on interaction of "Trikatu" with diclofenac sodium. | 2004 Apr |
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Effect of an indigenous herbal compound preparation 'Trikatu' on the lipid profiles of atherogenic diet and standard diet fed Rattus norvegicus. | 2004 Dec |
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Piperlonguminine from Piper longum with inhibitory effects on alpha-melanocyte-stimulating hormone-induced melanogenesis in melanoma B16 cells. | 2004 Dec |
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Immunomodulatory and antitumor effects in vivo by the cytoplasmic fraction of Lactobacillus casei and Bifidobacterium longum. | 2004 Mar |
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The PAV trial: does lactobacillus prevent post-antibiotic vulvovaginal candidiasis? Protocol of a randomised controlled trial [ISRCTN24141277]. | 2004 Mar 28 |
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A proteomic view of Bifidobacterium infantis generated by multi-dimensional chromatography coupled with tandem mass spectrometry. | 2005 May |
Sample Use Guides
In Vivo Use Guide
Sources: http://www.medicinform.net/spravka/s/s410.htm
Adults with acute diseases on day 1 - 1 g, then 200 mg / day. The duration of the course is 7-10 days. With chronic, long-term infections (with chronic lung diseases, rheumatism, kidney and urinary tract diseases) - 2 g in 1 dose once a week.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/137981
The bacteria Streptococcus faecium durans (Streptococcus faecalis ATCC 8043), Lactobacillus casei ATCC 7469, Pediococcus cereuisiae ATCC 8081, and Escherichia coli ATCC 10536 were used for activity evaluation. Amounts of 8 ml of the appropriate basal medium were placed in tubes and sterilized by autoclaving at 121 C for 10 min. Folic acid or calcium leucovorin diluted in 25% sterile glucose solution was added in 1-ml quantities. The final concentrations of folic acid were 0.002 ,ug/ml for S. faecium and 0.001 ,ug/ml for L. casei; the final concentration of calcium leucovorin was 0.001 ,ug/ml for P. cerevisiae. Stock solutions of PM in 0.04 N HCl and of CGT, TMP, and MTX in distilled water were sterilized by membrane filtration. SULFALENE dilutions in 1 ml of distilled water were added to give a final volume of 10 ml. Growth of the test organisms was read as turbidity in the Klett-Summerson photoelectric colorimeter. The results are expressed as the micromolar concentration required to produce 50% growth inhibition (ICs,) of the strain under the conditions used. Where sufficient drug was available, concentrations up to 1000 mkg/ml were tested; when this was not possible the highest concentration used was 100 mkg/ml.
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WHO-ATC |
J01ED02
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WHO-ATC |
P01BF04
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WHO-VATC |
QJ01EQ19
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NCI_THESAURUS |
C29739
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205-804-7
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DTXSID2046179
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CHEMBL1525826
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Sulfalene
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D013415
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110433
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10175
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m10312
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152-47-6
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DB00664
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T6BL4ZC15G
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2517
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9047
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100000085218
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SUB10705MIG
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C80793
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1209
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ACTIVE MOIETY