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| Author(s): |
Leticia Ribeiro de Assis
Total Authors: 1
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| Document type: | Master's Dissertation |
| Press: | São José do Rio Preto. 2017-06-21. |
| Institution: | Universidade Estadual Paulista (Unesp). Instituto de Biociências Letras e Ciências Exatas. São José do Rio Preto |
| Defense date: | 2017-06-02 |
| Advisor: | Luis Octavio Regasini; Fernando Rogério Pavan |
| Abstract | |
Tuberculosis (TB) is an infectious disease caused by Mycobacterium tuberculosis (MTB), wich is considered as a public health problem, due high number cases and deaths reported. Whereas a wide range of natural and synthetic chalconas (CHA) has presented activity against MTB, this study proposes the synthesis of new tuberculostatic-chalcone as molecular hybrids against MTB. Molecular hybrids were obtained in three stages: i) synthesis of chalcones; ii) synthesis of pirazinoic (PZA) and nalidixic (NDX) acid hydrazides; iii) synthesis of molecular pirazinamide-chalcone (PZA-CHA, serie I) and nalidixic acid-chalcone (NDX-CHA, serie II) hydrids. From reaction between chalcones and pirazinoic and nalidixic acid hydrazides were synthesized 26 new N-acylhydrazones. Among these, 13 from serie I and 13 from serie II with yields ranging from 4 to 63%. N-acylhydrazones were evaluated against Mycobacterium tuberculosis H37Rv ATCC 27294 strain. Among 26 evaluated molecular hybrids, para-methylated on ring B hybrid 61A (serie II) displayed potent activity against MTB at minimal inhibitory concentration of 37.1 µmol/L, evidencing hybridization molecular was efficient for anti-MTB chemical entity production. (AU) | |
| FAPESP's process: | 15/09969-0 - Preparation and Biological Evaluation of Tuberculostatic-Chalcone Hybrids as Potential Agents against Tuberculosis |
| Grantee: | Leticia Ribeiro de Assis |
| Support Opportunities: | Scholarships in Brazil - Master |