Novel antifungal 2-aryl-1-(1H-1,2,4-triazol-1-yl)butan-2-ol derivatives with high activity against Aspergillus fumigatus

Design, Synthesis, in vitro Antiproliferative Activity, Binding Modeling of 1,2,4,-Triazoles as New Anti-Breast Cancer Agents

“…Med spojinami sta 3 in 7 pokazali {irok spekter aktivnosti proti raku z IC50 vrednostmi 9.7 μM in 7.10 μM, njuna aktivnost pa je primerljiva s standardnimi zdravili. Molekulski model za vezavo med spojinami (1)(2)(3)(4)(5)(6)(7)(8) in aktivno mesto BRCA2 smo pridobili na osnovi rezultatov ra~unalni{kega sidranja in odnosom med strukturo in aktivnostjo.…”

“…Their important biological activities include antifungal, [1][2][3][4][5][6] antibacterial, 7 anticancer 8 and antiviral, [9][10][11] H1/H2 histamine receptor blockers, cholinesterase active agents, central nervous system (CNS) stimulants, antianxiety and sedatives. [12][13] Antimycotic, fluconazole, itraconazole, ravuconazole and variconazole are therapeutically interesting drug candidates, including 1,2,4-triazole nucleus.…”

Synthesis and comparison of bis(4-amino-5-mercapto-1,2,4-triazol-3-yl)butane using DFT study

“…Triazoles represent a very interesting class of compound because of their wide applications in pharmaceutical, analytical and industrial aspects, e.g. as antifungal [2][3][4][5], antibacterial [6], anticancer [7] and antiviral [8,9] and have biological activities [10,11]. The most effective corrosion inhibitors are those compounds containing heteroatom like nitrogen, oxygen, sulfur and phosphorus as well as aromatic rings.…”

Substituent effect of fluorine atoms in the 2,4-difluorophenyl group on antifungal activity of CS-758

“…Triazole derivatives displace lanosterol from lanosterol 14a-demethylase (14DM), a cytochrome P450-dependent enzyme, and block the biosynthesis of an essential component of fungal cell membrane, ergosterol [17]. In Japan, fluconazole [18] and itraconazole [19] have been the only triazole agents used clinically against systemic mycoses, and recently, voriconazole [20] has been launched on the market. Moreover, newer triazole agents, such as ravuconazole [21] and posaconazole [22] are reported to be under development (Fig.…”