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http://ir.cmu.edu.tw/ir/handle/310903500/28831
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| 題名: | BLOOD LEAD LEVELS IN THE GENERAL-POPULATION OF TAIWAN, REPUBLIC-OF-CHINA |
| 作者: | LIOU, SH;WU, TN;CHIANG, HC;YANG, GY;WU, YQ;LAI, JS;HO, ST;GUO, YL;KO, YC;CHANG, PY |
| 貢獻者: | 公共衛生學院環醫所;DEPT HLTH,TAIPEI,TAIWAN;TAIWAN PROV HSINCHU HOSP,DEPT FAMILY & OCCUPAT MED,HSINCHU,TAIWAN;CHINA MED COLL,INST ENVIRONM HLTH,TAICHUNG,TAIWAN;CHIA NAN JR COLL PHARM,DEPT IND SAFETY & HYG,TAINAN,TAIWAN;NATL CHENG KUNG UNIV,COLL MED,DEPT ENVIRONM & OCCUPAT HLTH,TAINAN,TAIWAN;KAOHSIUNG MED COLL,SCH PUBL HLTH,KAOHSIUNG,TAIWAN |
| 日期: | 1994 |
| 上傳時間: | 2010-09-24 13:57:30 (UTC+8) |
| 出版者: | SPRINGER VERLAG |
| 摘要: | A series of 2-substituted 3,4-dimethylfuro[2,3-c]pyrazole-5-carboxamides and related compounds have been synthesized and their antiallergic activities were evaluated. Most derivatives with a lower alkyl group at position 2 were orally active. Among them, N-ethyl-2,3,4-trimethylfuro[2,3-c]pyrazole-5-carboxamide (III3), 2-ethyl-N-methyl-3,4-dimethylfuro[2,3-c]pyrazole-5-carboxamide (III14), 2-isopropyl-N-methyl-3,4-dimethylfuro[2,3-c]pyrazole-5-carboxamide (III27), 5-(4,5-dihydro-5-oxo-1,3,4-oxadiazol-2-yl)-2,3,4-trimethylfuro[2,3-c]pyrazole (IV1) and 5-(4,5-dihgdro-5-oxo-1, 3,4-oxadiazol-2-yl)-2-isopropyl-3,4-dimethylfuro[2,3-c]pyrazole (IV3) showed promising antiallergic effects. The structure-activity relation of these 3,4-dimethylfuro[2,3-c]pyrazole derivatives was examined. An amide or 5-oxo-1,3,4-oxadiazole substituent at position 5 was favorable, while introduction of a carboxylic acid or acrylic acid moiety was unfavorable. However, none of these compounds exerted a significant inhibitory effect on mast cell degranulation. Compound III27 and IV3 showed potent anti-allergic activity. We found that they also suppressed histamine-, serotonin-, bradykinin- and substance P-induced ear edema in mice. In compound 48/80-pretreated mice, the preformed mediators in mast cells in the ear were greatly reduced. Under this condition, the bradykinin- and substance P-induced ear edema was suppressed by compound III27 and IV3 to a significantly greater extent than by diphenhydramine combined with methylsergide. These results indicated that the antiallergic effect of 3,4-dimethylfuro[2,3-c]pyrazole derivatives probably involves protection of the vasculature against the effects of challenge by several mediators. |
| 關聯: | INTERNATIONAL ARCHIVES OF OCCUPATIONAL AND ENVIRONMENTAL HEALTH 66(4):255-260 |
| 顯示於類別: | [環境醫學研究所(已停用)] 期刊論文
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