ERRATUMTo the article "4-Hydroxy-2-quinolones. 179. Synthesis, Structure, and Anti-inflammatory Activity of 4-Hydroxy-1-methyl-2-oxo-1,2-dihydroquinolin-3-ylacetic Acid and its Derivatives" -I.

Various methods of synthesizing amides of 2-hydroxy-4-imino-1,4-dihydroquinoline-3-carboxylic acids have been studied. Results of investigations on the antitubercular and antiinflammatory activity of the obtained compounds are discussed.Amides are a class of organic compounds which are rightfully considered to be most convenient for carrying out investigations devoted to the search for rules on structure-pharmacological activity links. The basis for such a conclusion is the fact that the amide group is an important component of many biologically active substances, both natural and synthetic. The enormous variety of methods and procedures used in the synthesis of amides, and also the practically unlimited selection of starting materials, enables systematic changes to be introduced into the structure of the final compounds, thereby purposefully changing their physicochemical and biological properties.Proceeding from this, one of the stages of our investigations was devoted to the amide of 4-amino-2-oxoquinoline-3-carboxylic acids. As one of the proposed variants of obtaining such compounds we studied the possibility of synthesizing amides of 1H-4-chloro-2-oxo-1,2-dihydroquinoline-3-carboxylic acid 1, which then might be transformed into the 4-amino derivative by any suitable method.Previous attempts to obtain amides 1 by the reaction of 4-chloro acid 2a with amines in the presence of N,N'-dicyclohexylcarbodiimide were unsuccessful [2]. Activation of the acid component of acid 2a with N,N'-carbonyldiimidazole (CDI) also gave no positive result. It turned out that on interacting 4-chloro-2-oxo-1,2-dihydroquinoline-3-carboxylic acid (2a) with N,N'-carbonyldiimidazole in anhydrous DMF the vigorous evolution of CO 2 characteristic of this reaction was observed, obviously indicating the formation of acylimidazole 3 (Scheme 1).

Until recently 4-hydroxyquinolin-2-ones have not even mentioned as analgesics in scientific literature. Only some years ago the situation turned over when based on preliminary virtual screening we obtained hydrochlorides of [(alkylamino)alkyl]amides of 1-allyl-4-hydroxy-6,7dimethoxy-2-oxo-1,2-dihydroquinoline-3-carboxylic acid as potential opioid receptor antagonists [24]. Further pharmacological research has confirmed the presence of "calculated" Pain and Treatment 22 Pain and Treatment 24 Pain and Treatment 28

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