YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
권호 표지

Synthesis and Analgesic-antiinflammatory Activity of Cinmetacin Derivatives

Cinmetacin유도체의 합성과 진통항염활성

  • 임채욱 (중앙대학교 약학대학 의약품화학 교실) ;
  • 이종민 (중앙대학교 약학대학 의약품화학 교실) ;
  • 유재학 (중앙대학교 약학대학 의약품화학 교실) ;
  • 이현수 (중앙대학교 약학대학 의약품화학 교실) ;
  • 임철부 (중앙대학교 약학대학 의약품화학 교실)
  • Published : 2001.02.01
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Abstract

Nine cinmetacin derivatives as potential nonsteroidal analgesic and antiinflammatory compounds were prepared and their analgesic-antiinflammatory activity was compared with cinmetacin. Salicylic acid and phenols were reacted with dicyclohexyl carbodiimide (DCC) to give phenol salicylates (1-4). Cinmetacin was treated with DCC and phenol derivatives to yield cinmetacin esters (5-13). Compounds (5, 7, 8, 10, 12, and 13) showed stronger analgesic activity than cinmetacin, but only compound (5) showed comparable antiinflammatory activity to cinmetacin.

Keywords

References

  1. Nonsteroidal Anti-ininflammatory Drugs Current Nonstelroidal Antiinflammatory Drug Therapy in Rheumatoid Arihritis, with Emphasis on Use in the Elderly Buchanan W. W;Kean W. F
  2. Pharmacology, Churchill living-stone(Third edition) Rang H. P.. Dale M. M;Ritter J. M
  3. Nonsteroidal antiin inflammatory Drugs(1st ed) Lombardino, J. G
  4. Am. J. Med v.77 Mechanism of action of nonsteroidal anti-inflammatory agents Goodwin, J. S
  5. J. Med. Chem v.12 1-Acylindoles. IX. Syntheses of 1-cinnamoyl-5-methoxy-2-methyl-3indolylaliphatic acids as potential antiinflammatory agents Yamamoto, H;Nakao, M
  6. Am. J. Med v.80 Effects of nonsteroidal anti-inflammatory drugs in healthy subjects Sedor, J. R., Davidson, E. W;Dunn, M. J
  7. Curr. Med. Res. Opin v.5 Endoscopic study of the gastro-intestinal tolerance of glucamethacin Mirelli, E., Fichera, G., Colpe, A. D;Lasala, M
  8. Curr. Med. Res. Opin v.12 Acemetacin and indomethacin in the treatment of rheumatoid arthritis: a double-blind comparative study in general practice Saul, P. A;Korlipara, K
  9. J. Pharm. Pharmacol v.32 Esterification of acidic anti-inflammatory drugs suppresses their gastrotoxicity without adversely affecting their antiinflammatory activity in rats Whitehouse, M. W;Rainsford, K. D
  10. J. Med. Chem v.23 Glycerides as prodrugs 3. Synthesis and antiinflammatory activity of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl] glycerides(indomethacin glycerides) Paris, G. Y., Garmaise, D. L., Cimon, D. G., Swett, L., Carter, G. W;Young. P
  11. Proc. Soc. Exp. Med v.111 Carrageenin-induced edema in hind paw of the rat as an assay for anti-inflammatory drugs Winter, C. A., Riskey, E. A;Nuss, G. W
  12. Fed. Proc v.18 Acetic acid for analgesic screening Koster, R., Anderson, M;De Beer, E. J