A.C. Valderrama – Negrón, Rocio I. Ramirez Panti, Christian M. Aliaga Paucar, Fernando Grandez Arias, Patricia Sheen Cortovaria, Mirko Juan Zimic Peralta, Yudith Cauna Orocollo
{"title":"Pyrazinamide–isoniazid hybrid: synthesis optimisation, characterisation, and antituberculous activity","authors":"A.C. Valderrama – Negrón, Rocio I. Ramirez Panti, Christian M. Aliaga Paucar, Fernando Grandez Arias, Patricia Sheen Cortovaria, Mirko Juan Zimic Peralta, Yudith Cauna Orocollo","doi":"10.15446/rev.colomb.quim.v50n3.96424","DOIUrl":null,"url":null,"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.","PeriodicalId":43662,"journal":{"name":"Revista Colombiana de Quimica","volume":" ","pages":""},"PeriodicalIF":0.2000,"publicationDate":"2022-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Revista Colombiana de Quimica","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.15446/rev.colomb.quim.v50n3.96424","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
引用次数: 0
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.
期刊介绍：
The Revista Colombiana de Química - Colombian Journal of Chemistry (Rev. Colomb. Quim.) Is a peer-reviewed scientific journal of the Department of Chemistry, Faculty of Sciences of the Universidad Nacional de Colombia, Bogotá. It currently publishes three volumes per year: January-April, May-August and September-December. All the content published by the Journal (available online) is under a Creative Commons attribution license type BY 4.0, that allows any person or entity in the world to freely access the content, share it, download it, adapt it or make derivative works without any restriction, provided that it adequately indicates the credit to the authors and to the Colombian Journal of Chemistry.
京公网安备 11010802042870号
京ICP备2023020795号-1
分享
求助内容：
应助结果提醒方式：
扫码关注我们
