Abstract
Tuberculosis remains one of the most common diseases affecting developing countries due to difficult living conditions, the rapidly increasing resistance of M. tuberculosis strains and the small number of effective anti-tuberculosis drugs. This study concerns the relationship between molecular structure observed in a solid-state by X-ray diffraction and the 15N NMR of a group of pyridine derivatives, from which promising activity against M. tuberculosis was reported earlier. It was found that the compounds exist in two tautomeric forms: neutral and zwitterionic. The latter form forced the molecules to adopt a stable, unique, flat frame due to conjugation and the intramolecular hydrogen bond system. As the compounds exist in a zwitterionic form in the crystal state generally showing higher activity against tuberculosis, it may indicate that this geometry of molecules is the “active” form.
Highlights
The widespread use of antibiotics in intensive livestock farming, the subsequent penetration of drugs and their metabolites into groundwater, and excessively and hastily prescribing antibiotics resulted in the emergence of many bacterial strains characterized by drug resistance [1]
A method developed at the Department of Organic Chemistry, Medical University of Gdańsk was used to obtain the methylimino ester, which consisted of carrying out the reaction in a methanol environment and diazabicyclo [5.4.0]undec-7-ene (DBU)
The synthesis of compounds 2–6 was described by the authors earlier [14]
Summary
The widespread use of antibiotics in intensive livestock farming, the subsequent penetration of drugs and their metabolites into groundwater, and excessively and hastily prescribing antibiotics resulted in the emergence of many bacterial strains characterized by drug resistance [1]. Increasing drug resistance among species of pathogenic bacteria poses a significant problem for the treatment of infectious diseases. One such disease is tuberculosis, caused by Mycobacterium tuberculosis [2]. Organization, 10 million people fell ill with tuberculosis in 2019 (including 1.2 million children under the age of 14), of which 1.4 million died. Only one in three patients entered treatment [3]
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