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Sinteza i farmakološko vrednovanje 2-supstituiranih-6-fenil-4,5-dihidropiridazin-3(2H)-ona kao snažnih srčanih stimulatora

Authors
Publisher
Croatian Pharmaceutical Society
Publication Date
Keywords
  • Piridazinoni
  • Anilidi
  • Derivati Hidrazina
  • Kardiotonično Djelovanje
  • Vazodilatacijsko Djelovanje
  • Pyridazinones
  • Anilides
  • Hydrazine Derivatives
  • Cardiotonic Activity
  • Vasodilatory Activity
Disciplines
  • Biology
  • Pharmacology

Abstract

The present study describes the synthesis and pharmacological evaluation of 2-substituted-6-(4-acylaminophenyl)-4,5-dihydropyridazin-3(2H)-ones as potent inodilating agents. The synthesis of target compounds 2-4 and 7-11 was acieved by Friedel-Crafts acylation of an appropriate anilide derivative with succinic anhydride or methylsuccinic anhydride and subsequent cyclization of intermediary keto acids with various hydrazine derivatives. The newly synthesized pyridazinone derivatives were evaluated for cardiotonic activity using isolated rat atria and for vasorelaxant activity using descending thoracic aortic rings of Wistar rats precontracted with phenylephrine (106 mol L1). 6-(4-Methanesulfonamidophenyl)-2-phenyl-4,5-dihydropyridazin-3(2H)-one (7) exhibited significant inodilatory properties and showed vasorelaxant activity in a nanomolar range (IC50 = 0.08  0.01 μmol L1).

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