Mofezolac Struktur

Mofezolac

Bezeichnung:Mofezolac

CAS-Nr78967-07-4

Englisch Name:Mofezolac

CBNumberCB7875698

SummenformelC19H17NO5

Molgewicht339.34

MOL-Datei78967-07-4.mol

Mofezolac physikalisch-chemischer Eigenschaften

Schmelzpunkt	147.5℃
Siedepunkt	527.2±50.0 °C(Predicted)
Dichte	1.250±0.06 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	DMSO: soluble
Aggregatzustand	A solid
pka	pKa ~3.3(at 25℃)
Farbe	White to off-white

Sicherheit

Toxizität

LD50 in male, female mice, male, female rats (mg/kg): 1528, 1740, 920, 887 orally; 275, 321, 378, 342 i.p.; 612, 545, 572, 510 s.c. (Satoh)

Gefahreninformationscode (GHS)

Mofezolac Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Mofezolac is a new non-steroidal analgesic antiinflammatory agent introduced in Japan for the treatment of post-operative and post-traumatic pain, acute upper respiratory tract pain, osteoarthritis, and lumbago. In in vfim studies, mofezolac inhibits prostaglandin biosynthesis and platelet aggregation, reportedly through the inhibition of cyclooxygenase. In animal studies, mofezolac showed more potent suppression in various writhing models than agents such as ibuprofen, mefenamic acid and aspirin. Mofezolac also has a potent inhibitory activity on the algesic responses induced by the mechanical stimulus of the inflamed tissue. The ulcerogenic effect of mofezolac on the gastric mucosa is far weaker than that of indomethacin and other agents.
Originator
Pasteur Merieux (France)
Definition
ChEBI: Mofezolac (TN) is a member of methoxybenzenes.
Trademarks
Disopain
Clinical Use
Yoshitomi (now Mitsubishi Pharma) has launched mofezolac, a COX-1 inhibitor with preferential COX-1 inhibition for the treatment of arthritis-related pain in Japan. The compound is used in oral doses of 75mg for the treatment of periarthritis, lumbago, neckshoulder- arm syndrome and pain after surgery, trauma, or dental extraction.
Synthese
The reaction of deoxyanisoin with hydroxylamine in methanol gives the corresponding 1,2-bis(4-methoxyphenyl)ethanone oxime, which is cyclized with ethyl acetate by means of n-butyllithium in tetrahydrofuran yielding 3,4-di(4-methoxyphenyl)-5-methylisoxazole. Finally, this compound is condensed with CO2 with n-butyllithium as catalyst in tetrahydrofuran to yield mofezolac . The synthesis with ClCO2C2H5 instead of CO2 is described in .

Mofezolac Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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