2-Aryl-5-benzoxazolealkanoic acid derivatives with notable antiinflammatory activity

Dw, Dunwell; Evans, D. D.; Ta, Hicks

doi:10.1021/jm00235a012

Cited by 57 publications

(16 citation statements)

References 3 publications

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“…Benoxaprofen 1 is a new nonsteroidal antiinflammatory agent [1] which has been recently introduced as an antirheumatic drug in Europe. Most nonsteroidal anti-inflammatory agents (NSAIA) that share the actions of analgesia and antipyresis attribute their mode of action to inhibition of prostaglandin synthesis [2].…”

Section: Introductionmentioning

confidence: 99%

Comparative effects of benoxaprofen and other anti-inflammatory drugs on bone damage in the adjuvant arthritic rat

Benslay

Nickander

1982

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Benoxaprofen, a new nonsteroidal anti-inflammatory agent recently marketed as an an antirheumatic drug, has been reported to suppress leucocyte migration into inflammatory sites, possibly by its reported inhibition of leukotriene synthesis. Benoxaprofen is also a weak to moderate inhibitor of prostaglandin synthesis. The effect of benoxaprofen was examined on adjuvant-induced arthritis in rats by radiographic assessment of bone damage. The effect of benoxaprofen was compared to other nonsteroidal anti-inflammatory agents, considered to act primarily by the inhibition of synthesis and/or release of prostaglandins. Drugs were administered from the 15th to the 30th day after induction of the adjuvant disease ('established adjuvant'). Radiographs of adjuvant rats showed extensive bone damage that was markedly suppressed by 30-40 mg/kg of benoxaprofen. Benoxaprofen exerted a dose-related inhibition of bone damage. There was less suppression of bone damage by comparable doses of phenylbutazone, oxyphenbutazone, ibuprofen, fenbufen, naproxen, tolectin and sulindac. Indomethacin, piroxicam and flurbiprofen were nearly as effective but only in doses that produced adverse effects or death in rats. Benoxaprofen may modify the progression of the experimental arthritic disease through a suppression of leucocyte migration.

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Section: Introductionmentioning

confidence: 99%

Comparative effects of benoxaprofen and other anti-inflammatory drugs on bone damage in the adjuvant arthritic rat

Benslay

Nickander

1982

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“…Benoxaprofen ( Figure 1) is a novel acidic compound (Dunwell, Evans, Hicks, Cashin & Kitchen, 1975) exhibiting notable anti-inflammatory, analgesic and antipyretic activity in animals (Cashin, Dawson & Kitchen, 1977). Single-dose studies in several animal species have shown that the compound is well absorbed after oral administration .…”

Section: Introduction Methodsmentioning

confidence: 99%

Preliminary studies of absorption and excretion of benoxaprofen in man.

Smith¹,

Goulbourn²,

Burt³

et al. 1977

Brit J Clinical Pharma

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1 Benoxaprofen is a new acidic anti‐inflammatory compound which was well absorbed after oral administration to man. 2 Single doses of 100, 200 and 400 mg produced mean peak concentrations in the plasma of 13.0, 33.5 and 45.3 microgram respectively, and the plasma half‐life of the compound was between 30 and 35 hours. 3 Multiple dosing with 25 and 50 mg every 24 h achieved an equilibrium conentration in the plasma after 6‐8 days, while dosing with 100 mg every 12 h enabled equilibrium to be reached in 3‐6 days. Plasma concentrations between 35 and 45 microgram/ml were achieved by giving 100 mg doses every 12 hours. 4 Absorption of benoxaprofen was delayed when the drug was given with food, but the total amount absorbed remained the same. 5 The effect of milling the material to small particle size (19 micron) was to increase the rate of absorption compared to that of unmilled material (58 micron). 6 Benoxaprofen was well tolerated by healthy male subject in the doses given.

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“…Benzoxazoles and other heterocycles are found in very important classes of bioactive compounds such as antibiotic, antibacterial, antiinflammatory, antistress, antiulcer, and anticancer agents [1][2][3][4][5][6][7]. They have recently received considerable attention for their pharmaceutical activities.…”

Section: Introductionmentioning

confidence: 99%