Abstract
A series of eight N-(disubstitutedbenzoyl)isoniazid derivatives have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv using the alamar blue susceptibility test and the activity expressed as the minimum inhibitory concentration (MIC) in μg/mL. Compounds 15 and 16 exhibited a significant activity (0.5 μg/mL) when compared with first line drugs such as isoniazid (INH) and rifampicin (RIP) and could be a good starting point to develop new lead compounds in the fight against multi-drug resistant tuberculosis.
Keywords: Isoniazid, analogs, anti-tubercular activity
Letters in Drug Design & Discovery
Title: Synthesis and In Vitro Anti-Tubercular Activity of a Series of N- (Disubstitutedbenzoyl)Isoniazid Derivatives
Volume: 3 Issue: 6
Author(s): Ivan Neves Junior, Maria C.S. Lourenco, Guilherme de B.P. de Miranda, Thatyana R.A. Vasconcelos, Karla C. Pais, Jose dos P. de A. Junior, M. S.V. Wardell, James L. Wardell and V. N. de Souza
Affiliation:
Keywords: Isoniazid, analogs, anti-tubercular activity
Abstract: A series of eight N-(disubstitutedbenzoyl)isoniazid derivatives have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv using the alamar blue susceptibility test and the activity expressed as the minimum inhibitory concentration (MIC) in μg/mL. Compounds 15 and 16 exhibited a significant activity (0.5 μg/mL) when compared with first line drugs such as isoniazid (INH) and rifampicin (RIP) and could be a good starting point to develop new lead compounds in the fight against multi-drug resistant tuberculosis.
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Neves Junior Ivan, Lourenco C.S. Maria, de Miranda de B.P. Guilherme, Vasconcelos R.A. Thatyana, Pais C. Karla, dos P. de A. Junior Jose, Wardell S.V. M., Wardell L. James and de Souza N. V., Synthesis and In Vitro Anti-Tubercular Activity of a Series of N- (Disubstitutedbenzoyl)Isoniazid Derivatives, Letters in Drug Design & Discovery 2006; 3 (6) . https://dx.doi.org/10.2174/157018006777805549
DOI https://dx.doi.org/10.2174/157018006777805549 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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