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 . 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.
Research on Chemical Intermediates – Springer Journals
Published: Sep 21, 2016
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