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Synthesis, structure and properties of N-aminosaccharin – A selective inhibitor of human carbonic anhydrase I. / Kuznetsov, Mikhail A.; Shestakov, Aleksandr N.; Zibinsky, Mikhail; Krasavin, Mikhail; Supuran, Claudiu T.; Kalinin, Stanislav; Tanç, Muhammet.

в: Tetrahedron Letters, Том 58, № 2, 2017, стр. 172-174.

Результаты исследований: Научные публикации в периодических изданияхстатьяРецензирование

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@article{f70d0b104ec0441a9e8d16b87c195b18,
title = "Synthesis, structure and properties of N-aminosaccharin – A selective inhibitor of human carbonic anhydrase I",
abstract = "Previously unknown N-aminosaccharin was prepared in good yield via the one-step direct amination of saccharin sodium salt with hydroxylamine-O-mesitylenesulfonic acid (MSH) and its reactivity investigated. N-aminosaccharin and its derivatives were tested against hCA isoforms and the parent compound was identified to be a selective, low micromolar inhibitor (Ki= 8.8 μM) of hCA I. These findings provide a ligand-efficient starting point for the design of potent hCA I inhibitors – a promising drug target for retinal/cerebral edema treatment.",
keywords = "hCA I inhibitor, Ligand efficiency, N-Amination, N-Aminosaccharin, Oxidative aminoaziridination",
author = "Kuznetsov, {Mikhail A.} and Shestakov, {Aleksandr N.} and Mikhail Zibinsky and Mikhail Krasavin and Supuran, {Claudiu T.} and Stanislav Kalinin and Muhammet Tan{\c c}",
note = "Publisher Copyright: {\textcopyright} 2016 Elsevier Ltd Copyright: Copyright 2018 Elsevier B.V., All rights reserved.",
year = "2017",
doi = "10.1016/j.tetlet.2016.12.005",
language = "English",
volume = "58",
pages = "172--174",
journal = "Tetrahedron Letters",
issn = "0040-4039",
publisher = "Elsevier",
number = "2",

}

RIS

TY - JOUR

T1 - Synthesis, structure and properties of N-aminosaccharin – A selective inhibitor of human carbonic anhydrase I

AU - Kuznetsov, Mikhail A.

AU - Shestakov, Aleksandr N.

AU - Zibinsky, Mikhail

AU - Krasavin, Mikhail

AU - Supuran, Claudiu T.

AU - Kalinin, Stanislav

AU - Tanç, Muhammet

N1 - Publisher Copyright: © 2016 Elsevier Ltd Copyright: Copyright 2018 Elsevier B.V., All rights reserved.

PY - 2017

Y1 - 2017

N2 - Previously unknown N-aminosaccharin was prepared in good yield via the one-step direct amination of saccharin sodium salt with hydroxylamine-O-mesitylenesulfonic acid (MSH) and its reactivity investigated. N-aminosaccharin and its derivatives were tested against hCA isoforms and the parent compound was identified to be a selective, low micromolar inhibitor (Ki= 8.8 μM) of hCA I. These findings provide a ligand-efficient starting point for the design of potent hCA I inhibitors – a promising drug target for retinal/cerebral edema treatment.

AB - Previously unknown N-aminosaccharin was prepared in good yield via the one-step direct amination of saccharin sodium salt with hydroxylamine-O-mesitylenesulfonic acid (MSH) and its reactivity investigated. N-aminosaccharin and its derivatives were tested against hCA isoforms and the parent compound was identified to be a selective, low micromolar inhibitor (Ki= 8.8 μM) of hCA I. These findings provide a ligand-efficient starting point for the design of potent hCA I inhibitors – a promising drug target for retinal/cerebral edema treatment.

KW - hCA I inhibitor

KW - Ligand efficiency

KW - N-Amination

KW - N-Aminosaccharin

KW - Oxidative aminoaziridination

UR - http://www.scopus.com/inward/record.url?scp=85006725073&partnerID=8YFLogxK

U2 - 10.1016/j.tetlet.2016.12.005

DO - 10.1016/j.tetlet.2016.12.005

M3 - Article

VL - 58

SP - 172

EP - 174

JO - Tetrahedron Letters

JF - Tetrahedron Letters

SN - 0040-4039

IS - 2

ER -

ID: 7738897