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 journalArticle

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 languageEnglish
Pages (from-to)6063-6072
Number of pages10
JournalBioorganic and Medicinal Chemistry
Volume17
Issue number16
DOIs
Publication statusPublished - Aug 15 2009

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Keywords

  • Hydrazone
  • Mycobacterium tuberculosis
  • Quinoline

ASJC Scopus subject areas

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

Cite this

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