Synthesis and Evaluation of Some Substituted Heterocyclic Fluconazole Analogues as Antifungal Agents

Abstract

During the past few decades, fungal infections are the commonly prevalent diseases from which a large proportion of the human population suffers 1-5. The increased emergence of both the superficial and systemic fungal infections has led to the massive increase in the rate of mortality, especially in the immuno-compromised individuals, those suffering from tuberculosis, cancer or AIDS 6,7. In clinic, azoles, especially triazole antifungal agents, were used most widely and efficiently. For example, fluconazole, voriconazole and itraconazole, presently play an important role in the treatment of fungal infections. However, their clinical use has been limited by the emergence of drug resistance, high risk of toxicity, insufficiencies in their antifungal activity and undesirable side effects 8-10. Hence, there is still a need to develop the safe and efficient chemotherapeutic agents with potent broad spectrum antifungal activities 10. EXPERIMENTAL Analytical TLC was carried out on Silica Gel 60 F254 plates (E. Merck) with detection by fluorescence and/or by charring with 10 % (v/v) H2SO4 in EtOH. Column chromatograph was performed on silica gel (200-300 mesh, Qindao Ocean Chemical Co., China). All chemicals and solvents were purchased from commercial sources unless specified otherwise. 1 H and 13 C NMR spectra were recorded in CDCl3, using

Flame Retardant Synergism of Bentonite and Magnesium Hydroxide in Polypropylene

“…Organo-bentonite, GK-4, was purchased from Jiangxi Gukang new materials Co. Ltd. Nano-magnesium hydroxide with average length of 193.9 nm and specific surface area of 22.4 m 2 /g was prepared using hydrothermal treatment 34 . Polypropylene, T30R, was supplied by Qilu Petrochemical Co. Ltd.…”

“…2 and Table-4 that, despite the initial decomposition temperature of S1 or S2 is slightly lower than that of S0, when the temperature exceeds 400 ºC, the mass loss of S1 or S2 is less than that of S0 at the same temperature. The purity magnesium hydroxide completely decomposes at 400 ºC for the magnesium oxide 34 . It can be found that, although the thermal stability of magnesium hydroxide is lower than that of polypropylene, the addition of magnesium hydroxide especially BT/MH improves the thermal stability of polypropylene, which further confirm the flame retardant synergism of bentonite and magnesium hydroxide in polypropylene.…”

Design and Synthesis of Antifungal Compounds from 1,2,3-Triazoles through the Click Chemistry Approach

“…An alternative strategy to increase the number of molecules in a chemical library from CuAAC reaction consists in changing the azide-alkyne group position on the reactive sites. With this idea, diverse alkynes were treated with 1-Azido-2-(2,4difluoro-phenyl)-3- [1,2,4]triazol-1-yl-propan-2-ol (9) yielding fluconazole analogues of type 10 [22][23][24]. All the compounds were highly active against different strains of fungi which prove that this kind of molecules possess an activity similar or higher than fluconazole having as further benefit that synthesis of these compounds is carried out with fewer reactions compared to the commercially available compound.…”