Abstract

RAMIREZ PANTI, Rocio I. et al. Pyrazinamide-isoniazid hybrid: synthesis optimisation, characterisation, and antituberculous activity. Rev.Colomb.Quim. [online]. 2021, vol.50, n.3, pp.16-23.  Epub July 20, 2022. ISSN 0120-2804.  https://doi.org/10.15446/rev.colomb.quim.v50n3.96424.

Over time, the effective resistance mechanisms to various first- and second-line drugs against the disease of tuberculosis make its treatment extremely difficult. This work presents a new approach to synthesizing a hybrid of antituberculosis medications: isoniazid (INH) and pyrazinamide (PZA). The synthesis was performed using ultrasound-assisted synthesis to obtain an overall yield of 70%, minimizing the reaction time from 7 to 1 h. The evaluation of the biological activity of the hybrid (compound 2) was tested using the tetrazolium microplate assay (TEMA), showing inhibition in the growth of Mycobacterium tuberculosis H37Rv at a concentration of 0.025 mM at pH 6.0 and 6.7.

Keywords : tuberculosis TEMA; MIC; ultrasound; isoniazid; pyrazinamide.

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