DOI

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.

Язык оригиналаанглийский
Страницы (с-по)172-174
Число страниц3
ЖурналTetrahedron Letters
Том58
Номер выпуска2
DOI
СостояниеОпубликовано - 2017

    Предметные области Scopus

  • Биохимия
  • Поиск новых лекарств
  • Органическая химия

ID: 7738897