Фармакокинетика и Фармакодинамика (Sep 2016)

Search selective blockers of the zinc-dependent metalloproteinases 2nd and 9th type among the benzoylamino (phenylsulfonyl) amino-substituted cyclic aminoacids derivatives

  • S. A. Kryzhanovskii,
  • G. V. Mokrov,
  • O. S. Grigorkevich,
  • I. B. Tsorin,
  • V. N. Stolyaruk,
  • M. B. Vititnova,
  • A. M. Likhosherstov,
  • T. A. Gudasheva

Journal volume & issue
Vol. 0, no. 3
pp. 3 – 8

Abstract

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The purpose of this study - search among the benzoylamino (phenyLsuLfonyL) amino-substituted cyclic aminoacids derivatives biologically active compounds exhibiting properties of the zinc-dependent metaLLproteinases 2nd and 9th type blockers which is known to pLay a key roLe in the pathogenesis of the myocardium earLy post-infarction remodeLing. In studying the effect of newLy synthesized compounds on metaLLoproteinase-9 LeveLs in bLood of rats with acute myocardiaL infarction were seLected compound Leader: 1-({4-[(4-chLorobenzoyL)amino]phenyL}suLfonyL-L-proLine, which effectiveLy bLocked the increase of this enzyme Level. Using echocardiography it was demonstrated that the seLected compound-Leader prevents the myocardiaL remodeLing deveLopment in the acute phase of experimentaL myocardiaL infarction, at Least not inferior to the reference inhibitor of metaLLoproteinases - doxycycLine.

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