吡嗪酰胺-异烟肼杂合物:合成优化、表征和抗结核活性

Pub Date : 2022-06-29 DOI:10.15446/rev.colomb.quim.v50n3.96424

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":"吡嗪酰胺-异烟肼杂合物:合成优化、表征和抗结核活性","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":0,"journal":{"name":"","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-06-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"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\":0,\"journal\":{\"name\":\"\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0,\"publicationDate\":\"2022-06-29\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"\",\"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\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"","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":"","JCRName":"","Score":null,"Total":0}

引用次数: 0

摘要

随着时间的推移，对各种针对结核病的一线和二线药物的有效耐药性机制使其治疗变得极其困难。这项工作提出了一种合成抗结核药物混合物的新方法：异烟肼（INH）和吡嗪酰胺（PZA）。使用超声辅助合成进行合成，以获得70%的总产率，使反应时间从7至1小时最小化。使用四氮唑微板测定法（TEMA）测试杂交体（化合物2）的生物活性的评估，显示在pH 6.0和6.7的0.025mM浓度下抑制结核分枝杆菌H37Rv的生长。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

查看原文

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

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.

求助全文

通过发布文献求助，成功后即可免费获取论文全文。去求助