Híbrido pirazinamida-isoniacida: Optimización de síntesis, caracterización y actividad antituberculosa

Rocio I. Ramirez Panti; Christian M. Aliaga Paucar; Fernando Grandez Arias; Patricia Sheen Cortovaria; Mirko Juan Zimic Peralta; Yudith Cauna Orocollo; Ana C. Valderrama Negron

doi:10.15446/rev.colomb.quim.v50n3.97095

Híbrido pirazinamida-isoniacida: Optimización de síntesis, caracterización y actividad antituberculosa

Rocio I. Ramirez Panti
, Christian M. Aliaga Paucar
, Fernando Grandez Arias
, Patricia Sheen Cortovaria
, Mirko Juan Zimic Peralta
, Yudith Cauna Orocollo
, Ana C. Valderrama Negron

Producción científica: Contribución a una revista › Artículo (Contribución a Revista) › revisión exhaustiva

2 Citas (Scopus)

Resumen

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.

Título traducido de la contribución	Pyrazinamide–isoniazid hybrid: synthesis optimisation, characterisation, and antituberculous activity
Idioma original	Español
Páginas (desde-hasta)	16-23
Número de páginas	8
Publicación	Revista Colombiana de Quimica
Volumen	50
N.º	3
DOI	https://doi.org/10.15446/rev.colomb.quim.v50n3.97095
Estado	Publicada - 2021
Publicado de forma externa	Sí

ODS de las Naciones Unidas

Este resultado contribuye a los siguientes Objetivos de Desarrollo Sostenible

ODS 3: Salud y bienestar

Palabras Clave

isoniazid
MIC
pyrazinamide
tuberculosis TEMA
ultrasound

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10.15446/rev.colomb.quim.v50n3.97095

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title = "H{\'i}brido pirazinamida-isoniacida: Optimizaci{\'o}n de s{\'i}ntesis, caracterizaci{\'o}n y actividad antituberculosa",

abstract = "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 = "isoniazid, MIC, pyrazinamide, tuberculosis TEMA, ultrasound",

author = "\{Ramirez Panti\}, \{Rocio I.\} and \{Aliaga Paucar\}, \{Christian M.\} and Arias, \{Fernando Grandez\} and Cortovaria, \{Patricia Sheen\} and Peralta, \{Mirko Juan Zimic\} and Orocollo, \{Yudith Cauna\} and \{Valderrama Negron\}, \{Ana C.\}",

note = "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 Ingenier{\'i}a 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: {\textcopyright} 2021, Universidad Nacional de Colombia. All rights reserved.",

year = "2021",

doi = "10.15446/rev.colomb.quim.v50n3.97095",

language = "Espa{\~n}ol",

volume = "50",

pages = "16--23",

journal = "Revista Colombiana de Quimica",

issn = "0120-2804",

publisher = "Universidad Nacional de Colombia",

number = "3",

}

Híbrido pirazinamida-isoniacida: Optimización de síntesis, caracterización y actividad antituberculosa. / Ramirez Panti, Rocio I.; Aliaga Paucar, Christian M.; Arias, Fernando Grandez et al.
En: Revista Colombiana de Quimica, Vol. 50, N.º 3, 2021, p. 16-23.

Producción científica: Contribución a una revista › Artículo (Contribución a Revista) › revisión exhaustiva

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 - https://www.scopus.com/pages/publications/85135294477

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 -

Híbrido pirazinamida-isoniacida: Optimización de síntesis, caracterización y actividad antituberculosa

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