Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone Derivatives
Two series of N’(E)-heteroaromatic-isonicotinohydrazide derivatives (3a-f and 4a-b) and 1-(7-chloroquinolin-4-yl)-2-[(heteroaromatic)methylene]hydrazone derivatives (5a-f and 6a-b) have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv....
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| Format: | Article |
| Language: | English |
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Wiley
2010-01-01
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| Series: | The Scientific World Journal |
| Online Access: | http://dx.doi.org/10.1100/tsw.2010.124 |
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| author | Marcelle de L. Ferreira Raoni S.B. Gonçalves Laura N. de F. Cardoso Carlos R. Kaiser Andre L.P. Candéa Maria das Graças M. de O. Henriques Maria C.S. Lourenço Flávio A.F.M. Bezerra Marcus V. N. de Souza |
| author_facet | Marcelle de L. Ferreira Raoni S.B. Gonçalves Laura N. de F. Cardoso Carlos R. Kaiser Andre L.P. Candéa Maria das Graças M. de O. Henriques Maria C.S. Lourenço Flávio A.F.M. Bezerra Marcus V. N. de Souza |
| author_sort | Marcelle de L. Ferreira |
| collection | DOAJ |
| description | Two series of N’(E)-heteroaromatic-isonicotinohydrazide derivatives (3a-f and 4a-b) and 1-(7-chloroquinolin-4-yl)-2-[(heteroaromatic)methylene]hydrazone derivatives (5a-f and 6a-b) have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv. Several compounds were noncytotoxic and exhibited significant minimum inhibitory concentration (MIC) activity (3.12, 2.50, 1.25, or 0.60 μg/mL), which can be compared to that of the first-line drugs ethambutol (3.12 μg/mL) and rifampicin (2.0 μg/ml). These results can be considered an important starting point for the rational design of new leads for anti-TB compounds. |
| format | Article |
| id | doaj-art-a8bdfe4a36c440278f6f88bb03e7f171 |
| institution | Kabale University |
| issn | 1537-744X |
| language | English |
| publishDate | 2010-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | The Scientific World Journal |
| spelling | doaj-art-a8bdfe4a36c440278f6f88bb03e7f1712025-02-03T01:09:27ZengWileyThe Scientific World Journal1537-744X2010-01-01101347135510.1100/tsw.2010.124Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone DerivativesMarcelle de L. Ferreira0Raoni S.B. Gonçalves1Laura N. de F. Cardoso2Carlos R. Kaiser3Andre L.P. Candéa4Maria das Graças M. de O. Henriques5Maria C.S. Lourenço6Flávio A.F.M. Bezerra7Marcus V. N. de Souza8FioCruz-Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos, Manguinhos, Rio de Janeiro, BrazilFioCruz-Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos, Manguinhos, Rio de Janeiro, BrazilFioCruz-Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos, Manguinhos, Rio de Janeiro, BrazilDepartamento de Química Orgânica, Instituto de Química, Universidade Federal do Rio de Janeiro, Rio de Janeiro, BrazilFioCruz-Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos, Manguinhos, Rio de Janeiro, BrazilFioCruz-Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos, Manguinhos, Rio de Janeiro, BrazilInstituto de Pesquisas Clínica Evandro Chagas – IPEC, Manguinhos, Rio de Janeiro, BrazilInstituto de Pesquisas Clínica Evandro Chagas – IPEC, Manguinhos, Rio de Janeiro, BrazilFioCruz-Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos, Manguinhos, Rio de Janeiro, BrazilTwo series of N’(E)-heteroaromatic-isonicotinohydrazide derivatives (3a-f and 4a-b) and 1-(7-chloroquinolin-4-yl)-2-[(heteroaromatic)methylene]hydrazone derivatives (5a-f and 6a-b) have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv. Several compounds were noncytotoxic and exhibited significant minimum inhibitory concentration (MIC) activity (3.12, 2.50, 1.25, or 0.60 μg/mL), which can be compared to that of the first-line drugs ethambutol (3.12 μg/mL) and rifampicin (2.0 μg/ml). These results can be considered an important starting point for the rational design of new leads for anti-TB compounds.http://dx.doi.org/10.1100/tsw.2010.124 |
| spellingShingle | Marcelle de L. Ferreira Raoni S.B. Gonçalves Laura N. de F. Cardoso Carlos R. Kaiser Andre L.P. Candéa Maria das Graças M. de O. Henriques Maria C.S. Lourenço Flávio A.F.M. Bezerra Marcus V. N. de Souza Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone Derivatives The Scientific World Journal |
| title | Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone Derivatives |
| title_full | Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone Derivatives |
| title_fullStr | Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone Derivatives |
| title_full_unstemmed | Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone Derivatives |
| title_short | Synthesis and Antitubercular Activity of Heteroaromatic Isonicotinoyl and 7-Chloro-4-Quinolinyl Hydrazone Derivatives |
| title_sort | synthesis and antitubercular activity of heteroaromatic isonicotinoyl and 7 chloro 4 quinolinyl hydrazone derivatives |
| url | http://dx.doi.org/10.1100/tsw.2010.124 |
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