The effects of long term D-penicillamine treatment on adjuvant arthritis in the rat were determined in order to establish a possible approach to the laboratory evaluation of anti-rheumatic drugs. Oral pretreatment (1-3 months) followed by continued through-treatment on a daily basis (100 mg/kg p.o.) failed to modify the parameters tested: viz. (a) body weight changes; (b) primary paw lesions; (c) secondary hind paw lesions; (d) secondary forepaw, ear and tail lesions; (e) the number of 'responders'. Autopsy showed no macroscopic abnormalities in the lungs, heart, thymus, liver, spleen, adrenal glands, kidneys and gastro-intestinal tract. These results are discussed in relation to previous findings whereby rat adjuvant arthritis, in addition to other experimental immune reactions, has been suggested as an indicator for D-penicillamine activity.

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A series of (4-substituted phenyl-1-piperazinyl)alkyl 2-aminobenzoates and 2-aminonicotinates has been prepared and screened for analgesic and antiinflammatory properties in mice and rats. The tabulated results reveal several 2-(4-substituted phenyl-1-piperazinyl)ethyl 2-(7- or 8-substituted 4-quinolinylamino)benzoates to be six to nine times more potent analgesics than the reference compounds (glafenine and aminopyrine) and to possess minor antinflammatory activity. Compound 45, 2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethyl 2-[[7-(trifluoromethyl)-4-quinolinyl]amino]benzoate (antrafenine), showed marked analgesic activity, long duration of action, and excellent tolerance in pharmacological and toxicological studies, as well as in clinical trials.

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Ausgehend von den Acetalestern (I) werden über die Intermediären (II), (III) und (V) die Derivate (VI) dargestellt, die nach einer modifizierten Bobbitt‐ Methode über die Dihydroisochinoline (VII) mit den Aldehyden (VIII) in die Papaverin‐Analogen (IX) übergeführt werden.