Microwave-assisted synthesis of 5-aryl-3-hydroxy-2-oxindole derivatives and evaluation of their antiglaucomic activity

Alexander M. Efremov,Denis A. Babkov,Olga Beznos,Elena Sokolova,Alexander A. Spasov,Vladimir N. Ivanov, Alexander Kurkin,Natalia B. Chesnokova,Natalia A. Lozinskaya

Mendeleev Communications（2023）

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摘要

A set of new 5-aryl-3-hydroxy-2-oxindoles was synthesized by decarboxylative condensation of the corresponding 5-aryl-substituted isatins with malonic or cyanoacetic acids under microwave irradiation. The antiglaucomic activity of the obtained compounds was evaluated. The most water soluble compounds can reduce the intraocular pressure (IOP) up to 2 Torr.

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关键词

oxindole,indolin-2-one,NRH,quinone oxidoreductase 2 inhibitors,intraocular pressure,antiglaucomic,microwave irradiation,condensation

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