Abstract
Purpose: This paper is dedicated to the investigation of cycloalkanecarbaldehydes, 1,2-benzoxathiin-4(3H)-on 2,2-dioxide and active methylene nitriles interaction and to studying antimicrobial properties of the obtained compounds.Methods: As initial products were used cycloalkanecarbaldehydes 1,2-benzoxathiin-4(3H)-on 2,2-dioxide and active methylene nitriles. During the course of the research were applied the methods of organic synthesis. The structures of the obtained compounds were confirmed by elemental analysis and 1H NMR spectroscopy. The antimicrobial activity was measured with the agar “well” diffusion method.Results: New 2-amino-4H-pyrans were synthesized by three-component reaction of cycloalkanecarbaldehydes, 1,2-benzoxathiin-4(3H)-on 2,2-dioxide and malononitrile. The replacement of the latter with ethylcyanoacetate in the case of cyclohexanecarbaldehyde led to the isolation of triethylammonium3-[(4-hydroxy-2,2-dioxido-2,1-benzoxathiin-3-yl)(cyclohexyl)methyl]-2,1-benzoxathiin-5-olat 2,2-dioxide. Based on this result and considering originality of such ammonium salts the latter were purposefully synthesized with two-component approach using a range of secondary and tertiary amines. The synthesized compounds demonstrated higher antimicrobial activity than the reference drugs against the gram-positive strains.Conclusions: The current research showed the prospective pathway for the expanding of the existing 2-amino-4H-pyrans diversity by utilizing in their synthesis such enolnucleophile and carbonyl compounds as 1,2-benzoxathiin-4(3H)-one 2,2-dioxide and cycloalkanecarbaldehydes respectively. The revealed antimicrobial activity of the obtained compounds against gram-positive microorganisms gives the opportunity for further investigations of narrow spectrum antibiotics among this group
Highlights
Nowadays the variety of organic compounds is absolutely tremendous
Corresponding multicomponent interactions generally proceed under reflux in polar solvents medium in the presence of basic catalysts, such as triethylamine, morpholine, piperidine [4]
Current investigations in this synthetic area are mainly focused on the selection of new reaction conditions and catalysts, and to search of some novel suitable components, that could replace well-known ones in order to expand the existing 2-amino-4H-pyrans diversity
Summary
The study of crops as sources of medicinal preparations obtaining on their basis is actual for pharmacy nowadays. Cabbage (Brassica oleracea L.) is a member of the family Brassicaceae (or Cruciferae). The complex of compounds contained in cabbage gives it many pharmacotherapeutic properties. In folk medicine of the West and the East cabbage has long been used against various diseases. The leaves, roots, stumps, and seeds of the plant are use [1]. Roots and stumps are considered as an antitumor agent [2, 3]. Folk medicine recommends that fresh leaves of cabbage can be applied to purulent wounds and ulcers, to the mammary glands during mastopathy. Cabbage leaves are used for abscess and other inflammatory diseases of the skin, including burns [3]. Fiber contained in cabbage improves the motor function of the intestines, shows positive influence on gut microflora.
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