Synthesis, characterization, POM analysis and antifungal activity of novel heterocyclic chalcone derivatives containing acylated pyrazole

Synthesis, characterization, POM analysis and antifungal activity of novel heterocyclic chalcone... Keywords Chalcone-pyrazole derivatives  Antifungal  Petra/Osiris/Molinspiration (POM) analyses  Pharmacophore site Identification Introduction Fungal infections are serious types of health problems infecting humans around the world [1]. The emergence of antibiotics to fight fungi and other microbes has resulted in the presence of pathogens that are resistant to pharmaceutical agents. The presence of drugs such as Fluconazole, Methotrexate, Azathioprine, Cyclosporine, Voriconazole, Itraconazole, Micafungin, Posaconazole, Flucytosine, Anidulafungin, Caspofungin and others can help to fight against fungal infections. Nevertheless, these drugs gave side effects when used in combination with other drugs [2, 3]. Therefore, pyrazole derivatives are some of the compounds that can act against fungi as they exhibit a broad range of pharmacological activities such as antibacterial, anticancer, antifungal, anti-inflammatory, anti-oxidant and others [4, 5]. The presence of a F–N interaction between fluoro-1 and the two nitrogen (N- 1 and N-2) atoms in the crystalline structure of Fluconazole [6–8] is an indication of the coexistence of two combined N,F-pharmacophore sites, and the removal or modification of this topology could obstruct or increase its various pharmacological activities (Fig. 1). Based on its diversity of biological activities, Flcuconazole has attracted our attention for the synthesis of bis-armed pyrazole derivatives 4a–h (Fig. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Research on Chemical Intermediates Springer Journals

Synthesis, characterization, POM analysis and antifungal activity of novel heterocyclic chalcone derivatives containing acylated pyrazole

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Publisher
Springer Netherlands
Copyright
Copyright © 2016 by Springer Science+Business Media Dordrecht
Subject
Chemistry; Catalysis; Physical Chemistry; Inorganic Chemistry
ISSN
0922-6168
eISSN
1568-5675
D.O.I.
10.1007/s11164-016-2737-y
Publisher site
See Article on Publisher Site

Abstract

Keywords Chalcone-pyrazole derivatives  Antifungal  Petra/Osiris/Molinspiration (POM) analyses  Pharmacophore site Identification Introduction Fungal infections are serious types of health problems infecting humans around the world [1]. The emergence of antibiotics to fight fungi and other microbes has resulted in the presence of pathogens that are resistant to pharmaceutical agents. The presence of drugs such as Fluconazole, Methotrexate, Azathioprine, Cyclosporine, Voriconazole, Itraconazole, Micafungin, Posaconazole, Flucytosine, Anidulafungin, Caspofungin and others can help to fight against fungal infections. Nevertheless, these drugs gave side effects when used in combination with other drugs [2, 3]. Therefore, pyrazole derivatives are some of the compounds that can act against fungi as they exhibit a broad range of pharmacological activities such as antibacterial, anticancer, antifungal, anti-inflammatory, anti-oxidant and others [4, 5]. The presence of a F–N interaction between fluoro-1 and the two nitrogen (N- 1 and N-2) atoms in the crystalline structure of Fluconazole [6–8] is an indication of the coexistence of two combined N,F-pharmacophore sites, and the removal or modification of this topology could obstruct or increase its various pharmacological activities (Fig. 1). Based on its diversity of biological activities, Flcuconazole has attracted our attention for the synthesis of bis-armed pyrazole derivatives 4a–h (Fig.

Journal

Research on Chemical IntermediatesSpringer Journals

Published: Sep 21, 2016

References

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