Abstract
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