作者: Hiromi Kataoka , Shizuyo Horiyama , Masae Yamaki , Hisae Oku , Kyoko Ishiguro
DOI: 10.1248/BPB.25.1436
关键词:
摘要: The anti-inflammatory activities of several novel oximes and O-acyl that we synthesized have been reported based on carrageenan-induced rat foot-pad swelling assay histamine-induced vascular permeability assay. A cyclooxygenase (COX)-1 inhibitory effect has also for 4′-piperidinoacetophenone 4′-morpholinoacetophenone their derivatives. To further search more effective non-steroidal or anti-allergic drugs, 1-hydroxylamino-1-(4′-piperidinophenyl) ethane (P-HA) 1-hydroxylamino-1-(4′-morpholinophenyl) (M-HA) were from the corresponding with sodium cyanoborohydride, N,O-diacetyl hydroxylamines (P-HA-Ac M-HA-Ac) prepared these using acetyl chloride. These clearly exhibited effects mouse induced by oral administration (150, 37.5 mg/kg). An dose P-HA-Ac (150 mg/kg) significantly inhibited anaphylactic reaction to ovalbumin measured abdominal wall (AW) method. Percutaneous P-HA M-HA 2,4-dinitrofluorobenzene (DNFB)-induced contact hypersensitivity (type IV) in mice at a 0.5 0.1 mg/ear, respectively. All tested both COX-1 COX-2 enzyme IC50 values 1.9—28.7 1.6—2.9 μM against COX-2, Hydroxylamines (P-HA M-HA) showed 5-lipoxygenase effect.