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In vivo and in vitro anti-inflammatory, antipyretic and ulcerogenic activities of pyridone and chromenopyridone derivatives, physicochemical and pharmacokinetic studies. | LitMetric

AI Article Synopsis

  • * We further enhanced these molecules by adding a chromene structure through a series of reactions, aiming to improve their biological properties.
  • * Initial tests showed that these new compounds have promising anti-inflammatory, ulcerogenic, and antipyretic effects, and we used computer modeling to predict their physical and biological characteristics compared to standard drugs like paracetamol and phenylbutazone.

Article Abstract

Throughout this study, we present the victorious synthesis of a novel class of 2(1H)-pyridone molecules, bearing a 4-hydroxyphenyl moiety through a one-pot reaction of 2-cyano-N-(4-hydroxyphenyl)acetamide with cyanoacetamide, acetylacetone or ethyl acetoacetate, and their corresponding aldehydes. In addition, the chromene moiety was introduced into the pyridine skeleton through the cyclization of the cyanoacetamide 2 with salicylaldehyde, followed by treatment with malononitrile, ethyl cyanoacetate, and cyanoacetamide, in order to improve their biological behaviour. Due to their anti-inflammatory, ulcerogenic, and antipyretic characters, the target molecules have undergone in-vitro and in-vivo examination, that display promising results. Moreover, in order to predict the physicochemical and ADME traits of all synthesized compounds and standard reference drugs, paracetamol and phenylbutazone, the in-silico prediction methodology was provided.

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Source
http://dx.doi.org/10.1016/j.bioorg.2021.104742DOI Listing

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