Amtolmetin guacil Struktur

Amtolmetin guacil

Bezeichnung:Amtolmetin guacil

CAS-Nr87344-06-7

Englisch Name:Amtolmetin guacil

CBNumberCB0129750

SummenformelC24H24N2O5

Molgewicht420.46

MOL-Datei87344-06-7.mol

Amtolmetin guacil physikalisch-chemischer Eigenschaften

Schmelzpunkt	117-120°
Siedepunkt	663.3±55.0 °C(Predicted)
Dichte	1.19±0.1 g/cm3(Predicted)
storage temp.	Sealed in dry,Room Temperature
Löslichkeit	DMSO (Slightly), Methanol (Slightly)
Aggregatzustand	Solid
pka	13.90±0.46(Predicted)
Farbe	Pale Brown to Light Brown
CAS Datenbank	87344-06-7(CAS DataBase Reference)

Sicherheit

Toxizität

LD50 in male mice, rats (mg/kg): 1370, 1100 i.p.; >1500, 1450 orally (Baglioni)

Gefahreninformationscode (GHS)

Amtolmetin guacil Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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)
Verwenden
Analgesic; anti-inflammatory used in the treatment of rheumatoid arthritis,
Definition
ChEBI: Amtolmetin guacil is a N-acyl-amino acid.
Trademarks
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 .
Synthese
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 guacil Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

87344-06-7, Amtolmetin guacil Verwandte Suche:

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