Posaconazole

Current Concepts in Antifungal Pharmacology

“…Voriconazole was shown to be more effective than conventional amphotericin B for the treatment of invasive aspergillosis 7 and is a useful agent for fusariosis, 8 whereas posaconazole had a spectrum of activity that included not only Aspergillus and Fusarium species but also many Mucorales. 9,10 Both agents could be administered orally, paving the way for their use not only for the treatment of suspected or documented mold infections but also as prophylaxis in severely immunocompromised patients. [11][12][13] Unfortunately, the broader spectrum of activity with triazole antifungal agents often comes at the expense of increased pharmacokinetic variability and risk of drug interactions.…”

A dried blood spots technique based LC–MS/MS method for the analysis of posaconazole in human whole blood samples

“…Posaconazole, marketed in the United States as Noxafil ® , is a triazole antifungal compound used to treat life threatening invasive fungal infections in immune suppressed patients [20]. Triazoles, such as posaconazole, are selective inhibitors of 14a-demethylase (CYP51) enzyme, leading to depletion of ergosterol and accumulation of 14a-methyl-sterols, thereby adversely affecting the fungal membrane synthesis [21].…”

Synthesis and biological activity of novel 1,3,5‐trisubstituted 1,2,4‐triazole derivatives

“…Physical (3). Methyl iodide (2.38 mL, 0.038 mol) was added to a stirred suspension of compound 2 (9.0 g, 0.031 mol) and anhydrous K 2 CO 3 (6.4 g, 0.046 mol) in DMF (50 mL) and stirred for 1 h at room temperature.…”

“…Although a large number of antibiotics and chemotherapeutics are available for medical use, the antimicrobial resistance created a substantial need of new class of antimicrobial agents in the last decades [1][2][3].…”