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
收藏
页码:16 / 23
页数:8
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