Abstract
A series of novel 5-aminosalicylic acid derivatives of various nonsteroidal anti-inflammatory drugs (diclofenac, ibuprofen, indomethacin, naproxen, and salicylic acid) was synthesized, and the conjugates were assayed for anti-inflammatory activity and gastrointestinal toxicity. All the new derivatives except the salicylic acid conjugate proved to be potent inhibitors of prostaglandin release in vitro. In the same assay, some of the new compounds also exhibited measurable anti-lipoxygenase activity; in no case was there a substantial increase in leukotriene production. Two of the new conjugates were tested in vivo for anti-inflammatory activity by standard methods. Such activity was observed in both rat carrageenin paw edema and rat adjuvant-induced arthritis model. In addition, several of the new compounds were tested for gastrointestinal toxicity in rats. The number of lesions observed was negligible in comparison with the controls receiving the respective parent compounds.
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