Modification of the Benzene Moiety in the Quinolone Nucleus of 4-Hydroxy-6,7-Dimethoxy-2-Oxo-N-(Pyridin-3-Ylmethyl)-1,2-Dihydroquinoline-3-Carboxamide as an Attempt to Enhance its Analgesic Activity

A series of close analogs of 4-hydroxy-6,7-dimethoxy-2-oxo- N -(pyridin-3-ylmethyl)-1,2-dihydroquinoline-3-carboxamide modified in the benzene moiety of the quinolone nucleus were synthesized to identify the structural fragments determining their analgesic effect. Results of pharmacological tests fo...

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Bibliographic Details
Published inPharmaceutical chemistry journal Vol. 52; no. 10; pp. 825 - 829
Main Authors Ukrainets, I. V., Mospanova, E. V., Bereznyakova, N. L., Davidenko, A. A.
Format Journal Article
LanguageEnglish
Published New York Springer US 2019
Springer
Subjects
Medicine
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
synthesis
amidation
4-hydroxy-2-oxo-1,2-dihydroquinoline-3-carboxamides
analgesic activity
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Summary:A series of close analogs of 4-hydroxy-6,7-dimethoxy-2-oxo- N -(pyridin-3-ylmethyl)-1,2-dihydroquinoline-3-carboxamide modified in the benzene moiety of the quinolone nucleus were synthesized to identify the structural fragments determining their analgesic effect. Results of pharmacological tests found that these chemical changes had a relatively weak influence on the analgesic activity of the tested compounds, leading to the conclusion that the modified fragment interacted insignificantly with the biological targets.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-019-1908-8