Результаты исследований: Научные публикации в периодических изданиях › статья › Рецензирование
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 изданиях › статья › Рецензирование
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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