Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies

Sandra Gemma; Luisa Savini; Maria Altarelli; Pierangela Tripaldi; Luisa Chiasserini; Salvatore Sanna Coccone; Vinod Kumar; Caterina Camodeca; Giuseppe Campiani; Ettore Novellino; Sandra Clarizio; Giovanni Delogu; Stefania Butini

doi:10.1016/j.bmc.2009.06.051

Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies

Sandra Gemma, Luisa Savini, Maria Altarelli, Pierangela Tripaldi, Luisa Chiasserini, Salvatore Sanna Coccone, Vinod Kumar, Caterina Camodeca, Giuseppe Campiani, Ettore Novellino, Sandra Clarizio, Giovanni Delogu, Stefania Butini

Research output: Contribution to journal › Article › peer-review

Abstract

A series of 4-quinolylhydrazones was synthesized and tested in vitro against Mycobacterium tuberculosis. At a concentration of 6.25 μg/mL, most of the newly synthesized compounds displayed 100% inhibitory activity against M. tuberculosis in cellular assays. Further screening allowed the identification of very potent antitubercular agents. Compound 4c was also tested in a time-course experiment and against mtb clinical isolates, displaying interesting results.

Original language	English
Pages (from-to)	6063-6072
Number of pages	10
Journal	Bioorganic and Medicinal Chemistry
Volume	17
Issue number	16
DOIs	https://doi.org/10.1016/j.bmc.2009.06.051
Publication status	Published - Aug 15 2009

Keywords

Hydrazone
Mycobacterium tuberculosis
Quinoline

ASJC Scopus subject areas

Pharmaceutical Science
Drug Discovery
Organic Chemistry
Molecular Medicine
Molecular Biology
Clinical Biochemistry
Biochemistry

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Gemma, S., Savini, L., Altarelli, M., Tripaldi, P., Chiasserini, L., Coccone, S. S., Kumar, V., Camodeca, C., Campiani, G., Novellino, E., Clarizio, S., Delogu, G., & Butini, S. (2009). Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies. Bioorganic and Medicinal Chemistry, 17(16), 6063-6072. https://doi.org/10.1016/j.bmc.2009.06.051

Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies. / Gemma, Sandra; Savini, Luisa; Altarelli, Maria; Tripaldi, Pierangela; Chiasserini, Luisa; Coccone, Salvatore Sanna; Kumar, Vinod; Camodeca, Caterina; Campiani, Giuseppe; Novellino, Ettore; Clarizio, Sandra; Delogu, Giovanni; Butini, Stefania.

In: Bioorganic and Medicinal Chemistry, Vol. 17, No. 16, 15.08.2009, p. 6063-6072.

Research output: Contribution to journal › Article › peer-review

Gemma, S, Savini, L, Altarelli, M, Tripaldi, P, Chiasserini, L, Coccone, SS, Kumar, V, Camodeca, C, Campiani, G, Novellino, E, Clarizio, S, Delogu, G & Butini, S 2009, 'Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies', Bioorganic and Medicinal Chemistry, vol. 17, no. 16, pp. 6063-6072. https://doi.org/10.1016/j.bmc.2009.06.051

Gemma, Sandra ; Savini, Luisa ; Altarelli, Maria ; Tripaldi, Pierangela ; Chiasserini, Luisa ; Coccone, Salvatore Sanna ; Kumar, Vinod ; Camodeca, Caterina ; Campiani, Giuseppe ; Novellino, Ettore ; Clarizio, Sandra ; Delogu, Giovanni ; Butini, Stefania. / Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies. In: Bioorganic and Medicinal Chemistry. 2009 ; Vol. 17, No. 16. pp. 6063-6072.

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abstract = "A series of 4-quinolylhydrazones was synthesized and tested in vitro against Mycobacterium tuberculosis. At a concentration of 6.25 μg/mL, most of the newly synthesized compounds displayed 100% inhibitory activity against M. tuberculosis in cellular assays. Further screening allowed the identification of very potent antitubercular agents. Compound 4c was also tested in a time-course experiment and against mtb clinical isolates, displaying interesting results.",

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AU - Chiasserini, Luisa

AU - Coccone, Salvatore Sanna

AU - Kumar, Vinod

AU - Camodeca, Caterina

AU - Campiani, Giuseppe

AU - Novellino, Ettore

AU - Clarizio, Sandra

AU - Delogu, Giovanni

AU - Butini, Stefania

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Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies

Abstract

Keywords

ASJC Scopus subject areas

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