3-Methyl-4-(((5-Nitrofuran-2-Yl)Methylene)Amino)Thiomorpholine 1,1-Dioxide 3-甲基-4-(((5-硝基呋喃-2-基)亚甲基)氨基)硫代吗啉-1,1-二氧化物

CAS 23256-30-6 MFCD00869254

化学结构图

23256-30-6
SMILES: CC1CS(=O)(=O)CCN1/N=C/C1=CC=C(O1)[N+]([O-])=O

化学属性

Mol. FormulaC10H13N3O5S
Mol. Weight287.32

别名和识别编码

Chemical Name3-Methyl-4-(((5-Nitrofuran-2-Yl)Methylene)Amino)Thiomorpholine 1,1-Dioxide
CAS Number23256-30-6
Synonym BAY 2502 Nifurtimox 3-Methyl-N-[(5-nitro-2-furanyl)methylene]- 4-((5-Nitrofurfurylidene)amino)-3-methylthiomorpholine-1,1-dioxide Lampit Tetrahydro-3-methyl-4-((5-nitrofurfurylidene)amino)-2H-1,4-thiazine Bayer 2502 1-((5-Nitrofurfurylidene)amino)-2-methyltetrahydro-1,4-thiazine-4,4-dioxide 3-Methyl-4-(5'-nitrofurylidene-amino)-tetrahydro-4H-1,4-thiazine-1,1-dioxide
Wiswesser Line NotationT6N DSWTJ B1 ANU1- BT5OJ ENW
Chemical Name Translation3-甲基-4-(((5-硝基呋喃-2-基)亚甲基)氨基)硫代吗啉-1,1-二氧化物
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分类

  • Heterocycles
  • Pharmaceuticals
  • Intermediates & Fine Chemicals
  • Sulfur & Selenium Compounds

产品应用

  • Antiprotozoal. Showing anti-Trypanosoma cruzi activity.

相关文献及参考

  • Letelier, M., et al.: Exp. Parasitol., 71, 357
  • [1]. Cabanillas Stanchi KM, et al. Nifurtimox reduces N-Myc expression and aerobic glycolysis in neuroblastoma. Cancer Biol Ther. 2015;16(9):1353-63.

安全信息

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Subcutaneous
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 11700 mg/kg/47W-I
TOXIC EFFECTS :
   Tumorigenic - equivocal tumorigenic agent by RTECS criteria
   Endocrine - thyroid tumors
   Skin and Appendages - tumors
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 22,1607,1972

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE/DURATION           : 11700 mg/kg/47W-I
TOXIC EFFECTS :
   Tumorigenic - equivocal tumorigenic agent by RTECS criteria
   Endocrine - adrenal cortex tumors
   Skin and Appendages - tumors
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 22,1607,1972

RTECSXM3020000
TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Mammal - cat
DOSE/DURATION           : >4 gm/kg
TOXIC EFFECTS :
   Behavioral - somnolence (general depressed activity)
   Gastrointestinal - nausea or vomiting
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 22,1590,1972

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rabbit
DOSE/DURATION           : 2 gm/kg
TOXIC EFFECTS :
   Details of toxic effects not reported other than lethal dose value
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 22,1590,1972

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Mammal - dog
DOSE/DURATION           : >2 gm/kg
TOXIC EFFECTS :
   Behavioral - convulsions or effect on seizure threshold
   Gastrointestinal - nausea or vomiting
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 22,1590,1972

TYPE OF TEST            : LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - mouse
DOSE/DURATION           : 2291 mg/kg
TOXIC EFFECTS :
   Behavioral - convulsions or effect on seizure threshold
REFERENCE :
   TRSTAZ Transactions of the Royal Society of Tropical Medicine and Hygiene.
   (Royal Soc. of Tropical Medicine and Hygiene, Manson House, 26 Portland Pl.,
   London W1N 4EY, UK)  V.14-    1920-  Volume(issue)/page/year: 74,43,1980

TYPE

TYPE OF TEST            : Cytogenetic analysis
ROUTE OF EXPOSURE       : Oral
TEST SYSTEM             : Rodent - rat
DOSE/DURATION           : 100 mg/kg/5D (Continuous)
REFERENCE :
   RBGED3 Revista Brasileira de Genetica.  Brazilian Journal of Genetics. (Dr.
   F.A. Moura Duarte, Dep. de Genetica, Faculdade de Medicina de Ribeirao
   Preto, 14.100 Ribeirao Preto, Sao Paulo, Brazil)  V.1-    1978-
   Volume(issue)/page/year: 4,357,1981

TYPE OF TEST            : DNA repair
TEST SYSTEM             : Bacteria - Escherichia coli
DOSE/DURATION           : 500 mg/L
REFERENCE :
   FOMIAZ Folia Microbiologica (Prague).  (Academia, Vodickova 40, 112 29
   Prague 1, Czechoslavakia) V.4-    1959-  Volume(issue)/page/year:
   25,388,1980

TYPE OF TEST            : Specific locus test
ROUTE OF EXPOSURE       : Oral
TEST

TYPE OF TEST            : Sperm Morphology
ROUTE OF EXPOSURE       : Oral
TEST SYSTEM             : Rodent - rat
DOSE/DURATION           : 100 mg/kg
REFERENCE :
   EXMPA6 Experimental and Molecular Pathology.  (Academic Press, Inc., 1 E.
   First St., Duluth, MN 55802)  V.1-    1962-  Volume(issue)/page/year:
   45,245,1986

TYPE OF TEST            : DNA damage
TEST SYSTEM             : Microorganism - not otherwise specified
DOSE/DURATION           : 100 umol/L
REFERENCE :
   BCPCA6 Biochemical Pharmacology.  (Pergamon Press Inc., Maxwell House,
   Fairview Park, Elmsford, NY 10523)  V.1-    1958-  Volume(issue)/page/year:
   34,1457,1985

TYPE OF TEST            : Mutation in microorganisms
TEST SYSTEM             : Bacteria - Salmonella typhimurium
DOSE/DURATION           : 5 ug/plate
REFERENCE :
   BJMRDK Brazilian Journal of Medical and Biological Research.  (Associacao
   Brasileira de Divulgacao Cientifica, Faculdade de Medicina de Ribeirao
   Preto, USP, 141000 Ribeirao Preto, SP, Brazil) V.14-    1981-
   Volume(issue)/page/year: 19,19,1986

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 2520 mg/kg
SEX/DURATION            : male 70 day(s) pre-mating
TOXIC EFFECTS :
   Reproductive - Fertility - male fertility index (e.g. # males impregnating
   females per # males exposed to fertile nonpregnant females)
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 22,1603,1972

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 500 mg/kg
SEX/DURATION

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - mouse
DOSE                    : 1250 mg/kg
SEX/DURATION            : female 6-15 day(s) after conception
TOXIC EFFECTS :
   Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death,
   e.g., stunted fetus)
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 22,1603,1972

TYPE OF TEST            : TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE       : Oral
SPECIES OBSERVED        : Rodent - rat
DOSE                    : 9100 mg/kg
SEX/DURATION            : male 91 day(s) pre-mating
TOXIC EFFECTS :
   Reproductive - Paternal Effects - spermatogenesis (incl. genetic material,
   sperm morphology, motility, and count)
   Reproductive - Paternal Effects - testes, epididymis, sperm duct
REFERENCE :
   ARZNAD Arzneimittel-Forschung. Drug Research.  (Editio Cantor Verlag,
   Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.)  V.1-    1951-
   Volume(issue)/page/year: 22,1590,1972

系列性分类


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