Amtolmetin guacil
Amtolmetin guacil Basic information
- Product Name:
- Amtolmetin guacil
- Synonyms:
-
- 2-(2-Methoxyphenyl)-2-(N-{1-Methyl-5-[(4-Methylphenyl)carbonyl]-1H-pyrrol-2-yl}acetaMido)acetate
- ArtroMed
- Eufans
- AMtolMethin Guacil
- AMtolMetin Guacyl
- N-[2-[1-Methyl-5-(4-Methylbenzoyl)-1H-pyrrol-2-yl]acetyl]glycine 2-Methoxyphenyl Ester
- 2-Methoxyphenyl 2-(2-(1-Methyl-5-(4-Methylbenzoyl)-1H-pyrrol-2-yl)acetaMido)acetate
- 2-methoxyphenyl1-methyl-5-p-methylbenzoylpyrrole-2-acetoamidoacetate
- CAS:
- 87344-06-7
- MF:
- C24H24N2O5
- MW:
- 420.46
- Product Categories:
-
- Aromatics
- Heterocycles
- Intermediates & Fine Chemicals
- Pharmaceuticals
- Mol File:
- 87344-06-7.mol
Amtolmetin guacil Chemical Properties
- Melting point:
- 117-120°
- Boiling point:
- 663.3±55.0 °C(Predicted)
- Density
- 1.19±0.1 g/cm3(Predicted)
- storage temp.
- Sealed in dry,Room Temperature
- solubility
- DMSO (Slightly), Methanol (Slightly)
- form
- Solid
- pka
- 13.90±0.46(Predicted)
- color
- Pale Brown to Light Brown
- CAS DataBase Reference
- 87344-06-7(CAS DataBase Reference)
Amtolmetin guacil Usage And Synthesis
Description
Amtolmetin guacil is an orally active non-steroidal antiinflammatory drug (NSAID) introduced for the treatment of osteoarthritis, rheumatoid arthritis and post-operative pain. Amtolmetin guacil is reported to elicit a more rapid and improved analgesic action than other agents such as paracetamol. In models of adjuvant arthritis and rheumatic diseases, amtolmetin guacil is more efficacious than existing drugs such as naproxen, indomethacin and piroxicam. As a non-acidic prodrug of tolmetin, it has similar in vivo activity to the parent but with minor ulcerogenic action, lower acute toxicity, and excellent biological and gastric tolerability.
Originator
Sigma Tau (Italy)
Uses
Analgesic; anti-inflammatory used in the treatment of rheumatoid arthritis,
Definition
ChEBI: Amtolmetin guacil is a N-acyl-amino acid.
brand name
Artromed
Clinical Use
Amtolmetin guacil (AMG) is a non-steroidal anti-inflammatory drug developed by Sigma-Tau for the treatment of pain and inflammation. It acts similarly to tolmetin, and in preclinical trials displayed long-lasting anti-inflammatory and analgesic activity. Amtolmetin has a good gastrointestinal tolerability in humans and does not induce gastric ulcers in the rat . The good gastrointestinal tolerability and even a gastroprotective effect was related to an increase of endogenous NO via stimulation of inducible NO synthase in the gastric mucosa .
Synthesis
The condensation of 1-methyl-
5-(4-methylbenzoyl)pyrrole-2-acetic acid with
glycine ethyl ester in the presence of carbonyldiimidazole
and triethylamine in tetrahydrofuran
gives the corresponding ethyl 2-acetate, which is hydrolyzed with
NaOH in tetrahydrofuran – water yielding 2-
-
acetamido]acetic acid. Finally, this compound is
esterified with 2-methoxyphenol (guaiacol) in
hot tetrahydrofuran with carbonyldiimidazole
as catalyst .
Amtolmetin guacilSupplier
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