Synthesis and Biological Properties of {[(4-Hydroxy-1-Methyl-2,2-Dioxido-1H-2,1-Benzothiazin-3-YL)Carbonyl]Amino}-Benzoic Acids and Their Derivatives


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Continuing the search for novel biologically active substances among the 4-hydroxy-2,2-dioxo-1H-2λ6,1-benzothiazine-3-carboxamides series, we report here the synthesis of a series of {[(4-hydroxy-1-methyl-2,2-dioxido-1H-2,1-benzothiazin-3-yl)carbonyl]amino} benzoic acids asd their derivatives at the carboxyl group. Pharmacological testing showed that compounds with a free carboxyl group are of interest as potential diuretics, while carbamide derivatives have potential as analgesics. Esterification of the carboxyl group with lower alkyl alcohols was less effective.

作者简介

I. Ukrainets

National Pharmaceutical University

Email: chem@folium.ru
乌克兰, Kharkov

L. Petrushova

Vinnitsa N. I. Pirogov National Medical University

Email: chem@folium.ru
乌克兰, Vinnitsa

S. Dzyubenko

Far East State Medical University

Email: chem@folium.ru
俄罗斯联邦, Khabarovsk

L. Grinevich

National Pharmaceutical University

Email: chem@folium.ru
乌克兰, Kharkov

G. Sim

Far East State Medical University

Email: chem@folium.ru
俄罗斯联邦, Khabarovsk

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