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

被引：1

作者：

Panti, Rocio I. Ramirez ^{[1
]}

Paucar, Christian M. Aliaga ^{[1
]}

Arias, Fernando Grandez ^{[1
]}

Cortovaria, Patricia Sheen ^{[2
]}

Peralta, Mirko Juan Zimic ^{[2
]}

Orocollo, Yudith Cauna ^{[2
]}

Negron, Ana C. Valderrama ^{[1
]}

机构：

[1] Univ Nacl Ingn, Biopolymer & Met Pharmaceut Res Lab LIBIPMET, Fac Sci, Lima, Peru

[2] Univ Peruana Cayetano Heredia, Bioinformat & Mol Biol Lab, Fac Sci & Philosophy, Lima, Peru

来源：

REVISTA COLOMBIANA DE QUIMICA | 2021年 / 50卷 / 03期

关键词：

tuberculosis TEMA; MIC; ultrasound; isoniazid; pyrazinamide; IN-VITRO; MYCOBACTERIUM; DERIVATIVES; DESIGN; ANTIMYCOBACTERIAL; SUSCEPTIBILITY; COMPLEXES; ASSAY; ACID;

D O I：

10.15446/rev.colomb.quim.v50n3.96424

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

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 H(37)Rv at a concentration of 0.025 mM at pH 6.0 and 6.7.

引用

页码：16 / 23

页数：8

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