Reisner D B, Ludwig B J, Stiefel F J, Gister S, Meyer M, Powell L S, Sofia R D
Arzneimittelforschung. 1977;27(4):760-6. doi: 10.1002/chin.197732244.
A series of 3,3a-dihydro-2H,9H-isoxazolo[3,2-b]-[1,3]benzoxazin-9-ones was synthesized and evaluated for anti-inflammatory, antipyretic and analgesic activity. Since many of these compounds exhibited promising activity, particularly in the anti-inflammatory tests, a number of homologous 2,3,4,4a-tetrahydro-10H-1,2-oxazino[3,2-b]-[1,3]benzoxazin-10-ones and one 3,4,5,5a-tetrahydro-2H, 11H,-1,2-oxazepino [3,2-b][1,3]benzoxazin-11-one, the 9-chloro analog, were also prepared and evaluated. The expanded ring members were generally less active than the tricyclic compounds containing the isoxazolidine ring.
合成了一系列3,3a-二氢-2H,9H-异恶唑并[3,2-b]-[1,3]苯并恶嗪-9-酮,并对其抗炎、解热和镇痛活性进行了评估。由于这些化合物中的许多都表现出有前景的活性,特别是在抗炎试验中,还制备并评估了一些同系的2,3,4,4a-四氢-10H-1,2-恶嗪并[3,2-b]-[1,3]苯并恶嗪-10-酮以及一种9-氯类似物3,4,5,5a-四氢-2H,11H,-1,2-恶唑并[3,2-b][1,3]苯并恶嗪-11-酮。扩环成员的活性通常低于含有异恶唑烷环的三环化合物。