Prakt. lékáren. 2005; 1(1): 16-17

Léčiva na bázi pyrazinu

doc. PharmDr. Martin Doležal Ph.D1,2
1 _
2 Farmaceutická fakulta, Hradec Králové

Synteticky připravené pyraziny jsou používány jako identická „vonidla“ či „chutidla“ v potravinářství, ve voňavkářství či v tabákovém průmyslu. Pyraziny mají celou škálu biologických účinků, používají se i jako důležitá léčiva. Historicky prvními byla sulfonamidová chemoterapeutika sulfapyrazin a jeho strukturní varianta sulfalen, velmi jednoduchým derivátem je stále významné antituberkulotikum pyrazinamid. Dalšími důležitými léčivy jsou kalium šetřící diuretikum amilorid, hypolipidemikum acipimox, perorální antidiabetikum glipizid či nebenzodiazepinové hypnotikum zopiklon. Z vyvíjených látek zaslouží pozornost potenciální antineoplastikum pyrazindiazohydroxid či zajímavé antivirotikum 6-fluor-3-hydroxypyrazin-2-karboxamid.

Keywords: Klíčová slova: pyrazin, chemická léčiva, vývoj léčiv.

Published: February 1, 2006  Show citation

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Doležal M. Léčiva na bázi pyrazinu. Praktické lékárenství. 2005;1(1):16-17.
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References

  1. A-Rahim YI, Beyer KHJr, Vesell ES. Studies on pyrazinoylguanidine. 3. Downregulation of lipolysis in isolated adipocytes. Pharmacology 1996; 53: 197-210. Go to original source... Go to PubMed...
  2. Bergmann KE, Cynamon MH, Welch JT. Quantitative structure-activity relationships for the in vitro antimycobacterial activity of pyrazinoic acid esters. J. Med. Chem. 1996; 39: 3394-3400. Go to original source... Go to PubMed...
  3. Bird CW. Heteroaromaticity. 5. A unified aromaticity index. Tetrahedron 1992; 48: 335-340. Go to original source...
  4. Doležal M, Jampílek J, Osička Z, a kol. Substituted 5-aroylpyrazine-2-carboxylic acid derivatives: synthesis and biological activity. Il Farmaco 2003; 58: 1105-1111. Go to original source... Go to PubMed...
  5. Duffield RM, Blum MS, Wheeler JW. Alkylpyrazine alarm pheromones in primitive ants with small colonial units. Comp. Biochem. Physiol. B 1976; 54: 439-440. In: Chem. Abstr. 1976; 85: 14043w. Go to original source... Go to PubMed...
  6. Edelman MJ, Meyers FJ, Grennan T, a kol. Phase II trial of pyrazine diazohydroxide in androgen-independent prostate cancer. Invest New Drugs. 1998; 16: 179-182. Go to original source... Go to PubMed...
  7. France CP, Winger G, Medzihradsky F, a kol. Mirfentanil - Pharmacological profile of a novel fentanyl derivative with opioid and nonopioid effects. J. Pharmacol. Exp. Ther. 1991; 258: 502-510.
  8. Furuta Y, Takahashi K, Fukuda Y, a kol. In vitro and in vivo activities of anti-influenza virus compound T-705 Antimicrob. Agents Chemother. 2002; 46: 977-981. Go to original source... Go to PubMed...
  9. Hocek M. Synthesis and biological activity of 2-and 6-C-substituted purine bases, nucleosides and acyclic nucleotide analogues. Chem. Listy 2002; 96: 978-982.
  10. Kessler FK, Ritter JK. Induction of a rat liver benzo[a]pyrene-trans-7,8-dihydrodiol glucuronidating activity by oltipraz and beta-naphthoflavone. Carcinogenesis 1997; 18: 107-114. Go to original source... Go to PubMed...
  11. Lee HS, Bastani B, Friedman L, a kol. Effect of the serotonin agonist, MK-212, on body temperature in schizophrenia. Biol. Psychiatry. 1992; 31: 460-470. Go to original source... Go to PubMed...
  12. Lüllmann H, Mohr K, Wehling M. Farmakologie a toxikologie. 1. české vydání Praha: Grada Publishing 2002: 696 s.
  13. Maga JA. Pyrazine update. Food Rev. Inter. 1992; 8: 479-558. Go to original source...
  14. McCullough KJ. Pyrazines and Related Ring Structures. In: Ansell MF. Rodd's Chemistry of Carbon Compounds. 2nd Edition, Vol. IV, Elsevier, New York, 1995: 93-130. Go to original source...
  15. Portnoy RCh. Arylthiodicyanopyrazines as plant disease control agents. U.S. 4, 113, 724 1978. In: Chem. Abstr. 1979; 90: P72233j.
  16. Prochaska HJ, Chavan SJ, Baron P, Polsky BJ. Oltipraz, a novel inhibitor of human-immunodeficiency-virus type1 (HIV-1) replication. Cell. Biochem. 1995; 22 Suppl.: 117-125. Go to original source... Go to PubMed...
  17. Tsai SJ, Jenq SN, Lee H. Naturally occurring diallyl disulfide inhibits the formation of carcinogenic heterocyclic aromatic amines in boiled pork juice. Mutagenesis 1996; 11: 235-240. Go to original source... Go to PubMed...
  18. Výzkumné záměry Ministerstva školství, mládeže a tělovýchovy ČR: MSM 0021620822.
  19. Woolfson A, Rothschild M. Speculating about pyrazines. Proc. Roy. Soc. Lond. Ser. B - Biol. Sci. 1990; 242: 113-119. Go to original source... Go to PubMed...




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