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

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 th...

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Main Authors: S. A. Kryzhanovskii, G. V. Mokrov, O. S. Grigorkevich, I. B. Tsorin, V. N. Stolyaruk, M. B. Vititnova, A. M. Likhosherstov, T. A. Gudasheva
Format: Article
Language:Russian
Published: LLC “Publisher OKI” 2016-09-01
Series:Фармакокинетика и Фармакодинамика
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Online Access:https://www.pharmacokinetica.ru/jour/article/view/176
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Summary: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.
ISSN:2587-7836
2686-8830