Pyrazinamide–isoniazid hybrid: synthesis optimisation, characterisation, and antituberculous activity

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.v50n3.96424

Pyrazinamide–isoniazid hybrid: synthesis optimisation, characterisation, and antituberculous activity

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

School of Science and Engineering

Universidad Nacional de Ingeniería
Universidad Peruana Cayetano Heredia

Research output: Contribution to journal › Article › peer-review

2 Scopus citations

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.

Translated title of the contribution	Híbrido pirazinamida-isoniacida: optimización de síntesis, caracterización y actividad antituberculosa
Original language	English
Pages (from-to)	16-23
Number of pages	8
Journal	Revista Colombiana de Quimica
Volume	50
Issue number	3
DOIs	https://doi.org/10.15446/rev.colomb.quim.v50n3.96424
State	Published - 2021

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

MIC
isoniazid
pyrazinamide
tuberculosis TEMA
ultrasound

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10.15446/rev.colomb.quim.v50n3.96424

Cite this

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title = "Pyrazinamide–isoniazid hybrid: synthesis optimisation, characterisation, and antituberculous activity",

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 = "MIC, isoniazid, 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.\}",

year = "2021",

doi = "10.15446/rev.colomb.quim.v50n3.96424",

language = "Ingl{\'e}s",

volume = "50",

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journal = "Revista Colombiana de Quimica",

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TY - JOUR

T1 - Pyrazinamide–isoniazid hybrid

T2 - synthesis optimisation, characterisation, and antituberculous activity

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.

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 - MIC

KW - isoniazid

KW - pyrazinamide

KW - tuberculosis TEMA

KW - ultrasound

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

U2 - 10.15446/rev.colomb.quim.v50n3.96424

DO - 10.15446/rev.colomb.quim.v50n3.96424

M3 - Artículo

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 -

Pyrazinamide–isoniazid hybrid: synthesis optimisation, characterisation, and antituberculous activity

Abstract

UN SDGs

Keywords

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