Antibacterial activity of Mannich bases derived from 2-naphthols, aromatic aldehydes and secondary aliphatic amines

Bioorg Med Chem Lett. 2016 May 15;26(10):2498-2502. doi: 10.1016/j.bmcl.2016.03.098. Epub 2016 Mar 28.

Abstract

A small library of 1-aminoalkyl 2-naphthols has been synthesized through the direct Mannich reaction of 2-naphthols with (hetero)aromatic aldehydes and secondary amines. All of the Mannich bases having a thiophen-2-yl ring in their structure had good activity against Gram-positive bacteria, irrespective of the nature of the amino moiety.

Keywords: Aminomethylation; Antibacterial; MRSA; Mannich base; Thiophene.

MeSH terms

  • Aldehydes / chemistry
  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology*
  • Drug Evaluation, Preclinical
  • Gram-Positive Bacteria / drug effects
  • Mannich Bases / chemistry*
  • Microbial Sensitivity Tests
  • Naphthols / chemistry
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology
  • Structure-Activity Relationship*

Substances

  • Aldehydes
  • Anti-Bacterial Agents
  • Mannich Bases
  • Naphthols
  • Small Molecule Libraries
  • 2-naphthol