Russian Chemical Bulletin

, Volume 61, Issue 10, pp 1969–1974 | Cite as

Novel 2-oxoquinoline-6-sulfonamides as thiazide-like diuretics

  • V. A. Zubkov
  • T. A. Tsapko
  • I. S. Gritsenko
  • A. L. Zagayko
  • L. V. Galuzinskaya
Full Articles


A series of novel N-aryl-7-chloro-4-methyl-2-oxo-1,2-dihydroquinoline-6-sulfonamides were obtained. The structure-activity relationship (SAR) approach was used to study their diuretic effect on rats. Diuretic activity was exhibited by all the test compounds, with 7-chloro-4-methyl-2-oxo-1,2-dihydroquinoline-6-sulfonanilide being most active. A SAR analysis revealed that the substituted (especially ortho-substituted in the benzene ring) arylamides diminish diuresis compared to the most active compound. For the most and least active compounds, their effects on the electrolyte excretion (Na+, K+, and Cl) and creatinine level were also studied.

Key words

quinolin-2-ones sulfonamides thiazide-like diuretics structure-activity relationship 


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Copyright information

© Springer Science+Business Media New York 2012

Authors and Affiliations

  • V. A. Zubkov
    • 1
  • T. A. Tsapko
    • 1
  • I. S. Gritsenko
    • 1
  • A. L. Zagayko
    • 1
  • L. V. Galuzinskaya
    • 1
  1. 1.National University of PharmacyKharkovUkraine

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