Antimycobacterial activity of new N(1)-[1-[1-aryl-3-[4-(1H-imidazol-1-yl)phenyl]-3-oxo]propyl]-pyridine-2-carboxamidrazone derivatives

Daniele Zampieri; Maria Grazia Mamolo; Luciano Vio; Maurizio Romano; Nataša Skoko; Marco Baralle; Valentina Pau; Alessandro De Logu

doi:10.1016/j.bmcl.2016.05.053

Antimycobacterial activity of new N(1)-[1-[1-aryl-3-[4-(1H-imidazol-1-yl)phenyl]-3-oxo]propyl]-pyridine-2-carboxamidrazone derivatives

Bioorg Med Chem Lett. 2016 Jul 15;26(14):3287-3290. doi: 10.1016/j.bmcl.2016.05.053. Epub 2016 May 19.

Authors

Daniele Zampieri¹, Maria Grazia Mamolo², Luciano Vio², Maurizio Romano³, Nataša Skoko⁴, Marco Baralle⁴, Valentina Pau⁵, Alessandro De Logu⁵

Affiliations

¹ Department of Chemistry and Pharmaceutical Sciences, Piazzale Europa 1, University of Trieste, 34127 Trieste, Italy. Electronic address: dzampieri@units.it.
² Department of Chemistry and Pharmaceutical Sciences, Piazzale Europa 1, University of Trieste, 34127 Trieste, Italy.
³ Department of Life Sciences, Via Valerio 28/1, University of Trieste, 34127 Trieste, Italy.
⁴ ICGEB, International Centre for Genetic Engeneering and Biootechnology, Padriciano 99, 34149 Trieste, Italy.
⁵ Department of Life and Enviromental Sciences, Via Porcell 4, University of Cagliari, 09124 Cagliari, Italy.

PMID: 27241693
DOI: 10.1016/j.bmcl.2016.05.053

Abstract

N(1)-[1-[1-aryl-3-[4-(1H-imidazol-1-yl)phenyl]-3-oxo]propyl]-pyridine-2-carboxamidrazone derivatives were design, synthesized and tested for their in vitro antimycobacterial activity. The new compounds showed a moderate antimycobacterial activity against the tested strain of Mycobacterium tuberculosis H37Ra and a significant antimycobacterial activity against several mycobacteria other than tuberculosis strains.

Keywords: Antimycobacterial activity; Mycobacteria other than tuberculosis (MOTT); Pyridine-2-carboxamidrazone derivatives.

MeSH terms

Anti-Bacterial Agents / chemical synthesis
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology*
Antifungal Agents / chemical synthesis
Antifungal Agents / chemistry
Antifungal Agents / pharmacology*
Bacteria / drug effects*
Dose-Response Relationship, Drug
Fungi / drug effects*
Imidazoles / chemical synthesis
Imidazoles / chemistry
Imidazoles / pharmacology*
Microbial Sensitivity Tests
Molecular Structure
Pyridines / chemical synthesis
Pyridines / chemistry
Pyridines / pharmacology*
Structure-Activity Relationship

Substances

Anti-Bacterial Agents
Antifungal Agents
Imidazoles
Pyridines