Authors: Jarrahpour, Aliasghar; Eskandari, Masoumeh; Zomorodian, Kamiar; Barati, Elham; Ashori, Raheleh; Salehi Vaziri, Mostafa; Pakshir, Keyvan

Source: Anti-Infective Agents in Medicinal Chemistry (Formerly Current Medicinal Chemistry - Anti-Infective Agents), Volume 9, Number 4, October 2010 , pp. 205-219(15)

Publisher: Bentham Science Publishers

Abstract:

The synthesis of 40 new monocyclic β-lactams bearing a morpholine moiety at their N1 positions is described. The structures of these compounds have been confirmed by IR, 1H-NMR, 13C-NMR, Mass spectra and Elemental analysis. The antimicrobial activities of the synthetic compounds have been tested against clinically important fungi including Candida, Aspergillus and Microsporum and Epidermophyton species by broth microdilution method as recommended by CLSI. Inhibition studies showed that some of the tested compounds, in particular those with phenoxy groups, exhibited strong antifungal activities against all tested fungi at concentrations of less than 8 μg/mL, while others only inhibited the growth of dermatophytes or Aspergillus species. These results suggest that the derivatives should be investigated further for possible use in antimicrobial products.

Keywords: Antifungal; aspergillus; azetidine-2-one; candida; dermatophyte; fungi; monocyclic β-lactam; morpholine; 1-(3-morpholinopropyl)-3-phenoxy-4-phenyl azetidin-2-one (6); Antifungal Susceptibility Testing; antifungal activity

Document Type: Research article

DOI: http://dx.doi.org/10.2174/187152110794785040

Publication date: 2010-10-01

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• Anti-Infective Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of new anti-infective agents.
  Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of current topics in anti-infective medicinal chemistry.
  
  Anti-Infective Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in anti-infective drug discovery.

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