Acyclic amine-carboxyboranes were effective anti-inflammatory agents in mice at 8 mg/kg x 2.
These amine-carboxyboranes were more effective than the standard indomethacin at 8 mg/kg x
2, pentoxifylline at 50 mg/kg x 2, and phenylbutazone at 50 mg/kg x 2. The heterocyclic amine
derivatives as well as amine-carbamoylboranes, carboalkoxyboranes, and cyanoboranes were
generally less active. However, selected aminomethyl-phosphonate-N-cyanoboranes
demonstrated greater than 60% reduction of induced inflammation. The boron compounds were
also active in the rat induced edema, chronic arthritis, and pleurisy screens, demonstrating
activity similar to the standard indomethacin. The compounds were effecive in reducing local
pain and decreased the tail flick reflex to pain. The derivatives which demonstrated good anti-inflammatory
activity were effective inhibitors of hydrolytic lysosomal, and proteolytic enzyme
activities with IC50 50
values equal to -6M
in mouse macrophages, human leukocytes, and Be
Sal osteofibrolytic cells. In these same cell lines, the agents blocked prostaglandin
cyclooxygenase activity with IC50 values of -6M. In mouse macrophage and human
leukocytes, 5′ lipoxygenase activity was also inhibited by the boron derivatives with IC50 values
of 10-6M. These IC50 values for inhibition of these enzyme activities are consistent with
published values of known anti-inflammatory agents which target these enzymes.
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