Synthesis and biological evaluation of carvacrol-based derivatives as dual inhibitors of H. pylori strains and AGS cell proliferation

This study reports on the synthesis, structural assessment, microbiological screening against several strains of H. pylori and antiproliferative activity against AGS cells of a large series of carvacrol-based compounds. Structural analysis consisted of elemental analysis, ¹H/¹³C/¹⁹F NMR spectra and crystallographic studies. Starting from these premises and keeping in mind that the development of drugs from plant secondary metabolites is a topic of the most recent ongoing research and engages large-scale pharmacological screenings of extracts and active compounds, we aimed at designing a large library of carvacrol-based derivatives possessing multiple tunable functional groups for their chemical modulation to desired properties and assuring the broadest chemical diversity. Indeed, natural product derivatives could shed light on new therapeutic agents against human diseases due to the modulation of the physical-chemical, toxicological and drug-like characteristics of their natural parent compound. This is very important when also addressing pathologies such as gastric cancer where a pluralism of causative factors must be faced by a feasible research strategy which can evolve a multi-targeted perspective (one molecule acting on separate targets of the disease). Moreover, this approach can overcome issue related to combination therapy and the possibility of drug-drug interactions. These newly synthesized compounds can be regarded as new lead compounds able to reduce H. pylori growth and to counteract the proliferation of AGS cells.

Author(s): Simone Carradori

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