Synthesis and evaluation of novel azoles as potent antifungal agents

Bioorganic & Medicinal Chemistry Letters
Liangjing LiQiuye Wu

Abstract

Using a rational approach to the design of antifungal agents, a series of azole agents with 1,3,4-oxadiazole side chains were designed and synthesized. The results of preliminary in vitro antifungal tests with eight human pathogenic compounds showed that all of the title compounds exhibited excellent activities against all of the tested fungi except Aspergillus fumigatus. Compounds 11e and 11f were found to be the most effective, with a minimum inhibitory concentration of 0.0039μg/mL, followed by voriconazole, which has a MIC of 0.0625μg/mL. The 1,3,4-oxadiazole side chain is not the major contributor but plays a role in eliciting the observed antifungal activity.

References

Nov 25, 2000·International Journal of Antimicrobial Agents·V T Andriole
May 2, 2008·Pharmacotherapy·John MohrLuis Ostrosky-Zeichner
Sep 17, 2008·Antimicrobial Agents and Chemotherapy·Guillermo Garcia-EffronDavid S Perlin
Oct 20, 2009·Revista iberoamericana de micología·Rafael Laniado-Laborín, Maria Noemí Cabrales-Vargas
Dec 3, 2009·JAMA : the Journal of the American Medical Association·Jean-Louis VincentUNKNOWN EPIC II Group of Investigators

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Citations

Aug 28, 2015·European Journal of Medicinal Chemistry·Mohammad ShaquiquzzamanMohammad Mumtaz Alam
Oct 17, 2018·Mini Reviews in Medicinal Chemistry·Garima VermaMohammad Shaquiquzzaman

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