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새로운 5-Fluorobenzimidazole 항진균제의 합성과 생물학적 평가

Synthesis and Biological Valutaion of New 5-Fluorobenzimidazole Antifungal Agents

  • 투고 : 2011.02.22
  • 심사 : 2011.03.18
  • 발행 : 2011.03.30

초록

New type of 5-fluorobenzimidazole derivatives was synthesized through the reaction of 4-fluoro-5-(2,6-dimethylmorpholinyl)-2-aminoaniline with 5-nitro-2-furoic acid and 5-methoxy-3-chlorobenzothiophene-2-carboxylic acid in presence of PPA and treatment of $OH^-$. the resulting substituted 5-fluorobenzimidazole derivatives(6), (7) was characterized by high solubility in common polar organic solvents. We considered 5-fluorobenzimidazole derivatives were useful especially for antifungal drugs. These results are discussed from the viewpoints of the chemical and physical structures of the 5-fluorobenzimidazole derivatives.

키워드

참고문헌

  1. Beneke, E. S. and Rogers, A, L. : Medical Mycology 4th. Ed., Burgess Pub. Co., p.1-8(1980).
  2. Finegold, S, M. and Baron, E. J. : Baily and Scotts Diagnostic Mincrobiology 7th Ed., The C.V. Mosby Co., p.678-774 (1986).
  3. R. J. Holt, Drugs, 9, 401(1972).
  4. E.P Goderfori, P. A. J. Janssen, C. A. M. Van Der Eyckem, A. H. M. T. Van Heertum, and C. J. E. Niemegeers, J. Med. Chem., 8, 220(1965). https://doi.org/10.1021/jm00326a017
  5. E. P. Goderfroi, J. Van Custsem, C. A. M. Van Der Eyckem, and P. A. J, Janssen, J. Med. Chem., 10, 1160(1967). https://doi.org/10.1021/jm00318a039
  6. R. Vanbreusegham, J. Van Cutsem, and D. Thienpont, Chemotherapy., 12, 107 (1967). https://doi.org/10.1159/000220494
  7. J. Van Cutsem and D. Thienpont, Chemotherapy., 17, 392(1972). https://doi.org/10.1159/000220875
  8. J.E. Bennett, Ann. Intern. Med., 73, 653 (1970). https://doi.org/10.7326/0003-4819-73-4-653
  9. K. H. Buchel, W. Draber, E. Regel, and M. Plempel, Arzeim-Forsch., 22, 1260 (1972).
  10. R. J. Holt, Drugs., 9, 401(1975). https://doi.org/10.2165/00003495-197509060-00001
  11. Heeres. R. J., Backy, J. J., Mostmans, J. H. and Van Gutsem, J : Antimycotic imidazole IV. Synthesis and antifungal activity of ketoconzole, a new ptent orally active broad-spectrum antifungal agent. J. Med. Chem. 22, 1003(1979). https://doi.org/10.1021/jm00194a023
  12. J. Van Cutsem and D. Thienopont, Preclinical Research Report R41 400/1. Janssen Pharmaceutica, Beeres, Belgium (1977).
  13. Goro Tsukamoto, Koihiro Yoshino, Toshihiko Kohno, J. Med. Chem. 23, 734-738(1980). https://doi.org/10.1021/jm00181a007