Benoxaprofen is a potent and long‐acting anti‐inflammatory and antipyretic compound. Its anti‐inflammatory activity has been demonstrated in carrageenan‐induced oedema, in cellulose pellet granuloma and in both developing and established adjuvant arthritis tests in rats. Its antipyretic activity is greater than either aspirin or paracetamol in tests inducing pyrexia with yeast or ‘E’ pyrogen in rats and rabbits. Benoxaprofen has analgesic activity in tests where pain is accompanied by inflammation but not in other experimental models of pain. The weak prostaglandin synthetase inhibiting properties of this compound differentiate it from other acid anti‐inflammatory compounds. The low ulcerogenic potential of benoxaprofen seen in animal models may be related to its relative inability to inhibit PG synthetase.

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Aus dem Cyclohexadien (I) und den isomeren Nitrilen (IIa) bzw. (IIb) werden die Cyanbicyclooctane (IIIa) bzw. (IIIb) synthetisiert, deren Reduktionsprodukte (IVa) bzw. (IVb) zu den Dimethylaminoderivaten (Va) bzw. (Vb) umgesetzt RI werden; die analog (IV) synthetisierten Aminomethylbicyclooctane (VI) werden nach einer modifizierten Eschweiler‐Clarke‐Methode zu den Derivaten (VII) N,N‐dimethyliert Die trans‐Diels‐Alder4Addukte (IX) ‐ zugänglich aus (I) und den trans‐Zimtaldehyden (VIII) ‐ werden durch Bromierung/Dehydrobromierung in die ungesättigten Aldehyde (X) übergeführt; Kondensation der Aldehyde (X) mit Methylamin gibt die entsprechenden Imine, die zu den sek. Aminen (XI) reduziert werden; diese lassen sich analog (VI) zu den tertiären Aminen (XII) umsetzen.

On the basis of these studies a protocol for conducting the DH reaction to MBSA was established and the activity of drugs on processes underlying the sensitization phase of the reaction or processes underlying the elieitation phase of the reaction have been examined. Steroid and immunosuppressant drugs were found to inhibit the DH footpad response when dosed during the sensitization whereas several 'specific-antl-rheumatlc' and 'immunoactlve' compounds were without effect, lndomethacin and sudoxi cam inhibited the DH reaction if dosed during the elieitatlon of the reaction but other non-steroidal anti-inflammatories tested did not significantly reduce the response. The clinically used anti-rheumatlc drugs D-peniciilamlne and levamisole did not inhibit the elicitation phase of the DH response but