ChemInform Abstract: 3‐PHENYL‐5‐(2,2,2‐TRIFLUORO‐1‐HYDROXY‐1‐(TRIFLUOROMETHYL)ETHYL)INDOLE‐2‐CARBONITRILE, A POTENT INHIBITOR OF PROSTAGLANDIN SYNTHETASE AND OF PLATELET AGGREGATION

Fahrenholtz, K. E.; Silverzweig, Mary Z.; Germane, H.; Crowley, Herman J.; Simko, B.; Dalton, Colin

doi:10.1002/chin.198016177

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“…Recently, Fahrenholtz et al (23) reported findings in which a certain agent had no ulcerogenic activity but did have inhibitory effects on prostaglandin biosynthesis.…”

Section: Resultsmentioning

confidence: 99%

Anti-inflammatory properties of a newly synthetized compound, 6-chloro-4-oxyimino-1-phenyl-1,2,3,4-tetrahydroquinoline (M-7074).

et al. 1981

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Abstract-Anti-inflammatoryproperties of a newly synthetized compound, 6-chloro-4-oxyimino-1-phenyl-1,2,3,4-tetrahydroquinoline (M-7074), have been investigated. Anti-edema activities of M-7074 were more potent than those of phenylbutazone in carrageenin, bradykinin and mustard edema tests in rats. M-7074 showed an inhibitory effect on adjuvant arthritis, especially on the secondary inflammatory lesions in rats. Inhibitory effect of M-7074 on cotton-pellet granuloma formation was all but equal to that of phenylbutazone in rats. M-7074 also showed inhibitory effects on ultraviolet erythema in guinea-pigs and increased vascular permeability in mice, moderate analgesic activity in rats and mice, and antipyretic activity in rats. Furthermore, inhibitory effects of M-7074 on prostaglandin biosynthesis in guinea-pig lung homogenate and arachidonic acid-induced aggregation of rabbit platelets were fairly equal to those of indomethacin. However, M-7074 showed no effect on humoral nor cellular immunity in mice. M-7074 possessed no ulcerogenic activity in rats and mice, and LD50 value of M-7074 was 8.01 g/kg, p.o. in mice. These data indicate that M-7074 is a novel anti-inflammatory agent with large margin of safety.6-chloro-4-oxyimino-1-phenyl-1,2,3,4 tetrahydroquinoline (M-7074) shown in Fig.

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“…Recently, Fahrenholtz et al (23) reported findings in which a certain agent had no ulcerogenic activity but did have inhibitory effects on prostaglandin biosynthesis.…”

Section: Resultsmentioning

confidence: 99%

Anti-inflammatory properties of a newly synthetized compound, 6-chloro-4-oxyimino-1-phenyl-1,2,3,4-tetrahydroquinoline (M-7074).

et al. 1981

View full text Add to dashboard Cite

show abstract

ChemInform Abstract: 3‐PHENYL‐5‐(2,2,2‐TRIFLUORO‐1‐HYDROXY‐1‐(TRIFLUOROMETHYL)ETHYL)INDOLE‐2‐CARBONITRILE, A POTENT INHIBITOR OF PROSTAGLANDIN SYNTHETASE AND OF PLATELET AGGREGATION

Abstract: Die Diazoniumverbindung (I) reagiert mit dem Ketocarbonsäureester (II) über (III) und (IV) zum Indol (V) und Pyrazolon (VI).

Cited by 1 publication

References 1 publication

Anti-inflammatory properties of a newly synthetized compound, 6-chloro-4-oxyimino-1-phenyl-1,2,3,4-tetrahydroquinoline (M-7074).

Anti-inflammatory properties of a newly synthetized compound, 6-chloro-4-oxyimino-1-phenyl-1,2,3,4-tetrahydroquinoline (M-7074).

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