Synthesis of isoniazid-aldehyde codrugs and their activities against multidrug-resistant mycobacterium tuberculosis
Date of Completion
Bachelor of Science in Biochemistry
In response to the need for drugs to combat multidrug-resistant tuberculosis (MDR-TB), four isoniazid-aldehyde derivatives have been synthesized, characterized and tested as antimycobacterial agents. The prepated imines were characterized by spectroscopy, FT-IR spectroscopy, HPLC, and 1H and 13C NMR spectroscopy. the expected structure of N'-[(E)-(4-medthoxyphenyl)methylene]isonicotinohydrazide and N'-[(1E,2Z)-2-bromo-3-phenyl-2propen-1ylidene]isonicotinohydrazide agress with their 1H and13C NMR spectra. Minimum inhibitory concentrations (MIC) of the four products against MDR-TB strain were determined using resazurin mictotiter assay (REMA). The codrugs were found to be less active compared to reference drugs isoniazid, ofloxacin and levofloxacin. For the first time, p-anisaldehyde and and a-bromocinnamaldehyde were reported to have an activity against MDR-TB. Furthermore, a-bromocinnamaldehyde was found to be more active than isoniazid.
Narvaez, J. D., Orongan, J. L., & Pascua, J. P. (2018). Synthesis of isoniazid-aldehyde codrugs and their activities against multidrug-resistant mycobacterium tuberculosis. Retrieved from https://greenprints.dlshsi.edu.ph/bch/62