TY - JOUR
T1 - Híbrido pirazinamida-isoniacida
T2 - Optimización de síntesis, caracterización y actividad antituberculosa
AU - Ramirez Panti, Rocio I.
AU - Aliaga Paucar, Christian M.
AU - Arias, Fernando Grandez
AU - Cortovaria, Patricia Sheen
AU - Peralta, Mirko Juan Zimic
AU - Orocollo, Yudith Cauna
AU - Valderrama Negron, Ana C.
N1 - Funding Information:
This work was financially supported by Management Agreement No. 208-2015-FONDECYT to the Vice-Rectorate of Research of the Universidad Nacional de Ingeniería and the Ministry of Education of Peru. We would like to thank Dra. Maribel Navarro Acosta (Biometal Pharmaceutical and Catalysis Laboratory, Juiz de Fora, Minas Gerais, Brazil) who recorded the nuclear magnetic resonance spectra and elemental analysis.
Publisher Copyright:
© 2021, Universidad Nacional de Colombia. All rights reserved.
PY - 2021
Y1 - 2021
N2 - 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.
AB - 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.
KW - isoniazid
KW - MIC
KW - pyrazinamide
KW - tuberculosis TEMA
KW - ultrasound
UR - http://www.scopus.com/inward/record.url?scp=85135294477&partnerID=8YFLogxK
U2 - 10.15446/rev.colomb.quim.v50n3.97095
DO - 10.15446/rev.colomb.quim.v50n3.97095
M3 - Artículo (Contribución a Revista)
AN - SCOPUS:85135294477
SN - 0120-2804
VL - 50
SP - 16
EP - 23
JO - Revista Colombiana de Quimica
JF - Revista Colombiana de Quimica
IS - 3
ER -
