Synthesis and biological evaluations of enoxacin carboxamide derivatives

M. Saeed Arayne, Najma Sultana, Urooj Haroon, Osman Mesaik Mohammed Ahmed Hassan, Muhammad Asif

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

The present work deals with the synthesis of various enoxacin analogues via nucleophilic substitution of 3-carboxylic acid moiety of the drug by aromatic amines. The free carboxylic group was utilized in the formation of amides and the effect of functional group exchange on different biological activities of the parent was evaluated. The structure of these derivatives was established by various spectroscopic techniques and mass spectrometry. The derivatives were evaluated as antibacterial agents against a series of Gram-positive and Gram-negative bacteria whereby some of them displayed considerably improved antimicrobial profile against Gram-negative test strains. Additionally unlike enoxacin, the derivatives were also found to modulate oxidative burst response of phagocytes exhibiting moderate to significant inhibitory activity.

Original languageEnglish
Pages (from-to)967-974
Number of pages8
JournalArchives of Pharmacal Research
Volume32
Issue number7
DOIs
Publication statusPublished - Jul 2009
Externally publishedYes

Fingerprint

Enoxacin
Derivatives
Respiratory Burst
Phagocytes
Carboxylic Acids
Gram-Negative Bacteria
Amides
Amines
Mass Spectrometry
Anti-Bacterial Agents
Bioactivity
Functional groups
Mass spectrometry
Bacteria
Substitution reactions
Pharmaceutical Preparations

Keywords

  • Antibacterial activity
  • Derivatives
  • Enoxacin
  • Nucleophilic substitution
  • Oxidative burst response

ASJC Scopus subject areas

  • Drug Discovery
  • Molecular Medicine
  • Organic Chemistry

Cite this

Synthesis and biological evaluations of enoxacin carboxamide derivatives. / Saeed Arayne, M.; Sultana, Najma; Haroon, Urooj; Mohammed Ahmed Hassan, Osman Mesaik; Asif, Muhammad.

In: Archives of Pharmacal Research, Vol. 32, No. 7, 07.2009, p. 967-974.

Research output: Contribution to journalArticle

Saeed Arayne, M. ; Sultana, Najma ; Haroon, Urooj ; Mohammed Ahmed Hassan, Osman Mesaik ; Asif, Muhammad. / Synthesis and biological evaluations of enoxacin carboxamide derivatives. In: Archives of Pharmacal Research. 2009 ; Vol. 32, No. 7. pp. 967-974.
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