YAKHAK HOEJI (약학회지)
- Volume 34 Issue 2
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- Pages.126-132
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- 1990
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- 0377-9556(pISSN)
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- 2383-9457(eISSN)
Studies of Pharmacological Activity on the Piperazine Derivatives of Ibuprofen
이부프로펜의 피페라진 유도체에 대한 약리활성연구
- Jo, Han-Jin (College of Pharmacy, Chungnam National University) ;
- La, Sung-Bum (College of Pharmacy, Chungnam National University) ;
- Nam, Sang-Cheol (College of Pharmacy, Chungnam National University) ;
- Park, Mork-Soon (College of Pharmacy, Chungnam National University) ;
- Jee, Ung-Kil (College of Pharmacy, Chungnam National University)
- Published : 1990.04.30
Abstract
To enhance the activity of ibuprofen, amides of ibuprofen, 1-piperazinyl-2-(4-isobutylphenyl)propionamide(Ibu-P.A.) and 1-(4-methylpiperazinyl)-2-(4-isobutylphenyl)propionamide (Ibu-M.P.), were synthesized and the pharmaceutical properties and the pharmacological activities of the amides were studied. The lipid:water partition coefficients and pKa values were examined in vitro, and the antiinflammatory effect, analgesic effects, acute toxicity, and intestinal absorption were studied for the amides and compared with ibuprofen in vivo. The results are summarized as belows; 1) The lipid:water partition coefficients of Ibu-M.P. were higher than those of ibuprofen. 2) The calculated pKa values of ibuprofen and Ibu-M.P. were 5.49 and 8.66, respectively. 3) The antiinflammatory effects of ibuprofen, Ibu-P.A., and Ibu-M.P. were same intensity, but the duration of the effects of Ibu-P.A. and Ibu-M.P. were longer than that of ibuprofen. 4) The analgesic effect of Ibu-M.P. was more potent than those of ibuprofen and Ibu-P.A. in the acetic acid-induced writhing test. 5) The
Keywords
- Ibuprofen;
- piperazine anhydrous;
- 1-methylpiperazine;
- lipid: water partition coefficient;
- pka value;
- antiinflammatory effect;
- analgesic effect;
- $LD_{50}$;
- intestinal absorption