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ID: ALA5247666
Journal: Bioorg Med Chem Lett
Title: The rational design of novel 5-amino-2-oxindole derivatives with antiglaucomic activity.
Authors: Eremeev RO, Beznos OV, Efremov AM, Chesnokova NB, Lozinskaya NA.
Abstract: Compounds with a 2-oxindole scaffold play an important role in organic synthesis and especially in the synthesis of bioactive organic compounds, therefore, the development of new methods for modifying this scaffold is a very interesting and urgent task. In the framework of this study, we have created a rational approach to the synthesis of 5-amino-substituted derivatives of 2-oxindole. The approach is characterized by good total yield and a small number of steps. One-stage modification of obtained 5-amino-2-oxindoles leads to compounds with promising antiglaucomic activity. The most active compound 7a reduce intraocular pressure by 24% in normotensive rabbits (18% for reference drug timolol).
CiteXplore: 37207847