58905-24-1

Upstream product

• 41011-01-2 2-bromo-1-(3-chloro-phenyl)-ethanone 
• 99-02-5 3'-Chloroacetophenone 
• 288-88-0 1,2,4-Triazole 

Downstream Products

• 936105-07-6 4-(3-chloro-phenyl)-5-[1,2,4]triazol-1-yl-thiazol-2-ylamine 

Relevant academic research and scientific papers

Novel alkylated azoles as potent antifungals

Fluconazole (FLC) is the drug of choice when it comes to treat fungal infections such as invasive candidiasis in humans. However, the widespread use of FLC has resulted in the development of resistance to this drug in various fungal strains and, simultaneously has occasioned the need for new antifungal agents. Herein, we report the synthesis of 27 new FLC derivatives along with their antifungal activity against a panel of 13 clinically relevant fungal strains. We also explore their toxicity against mammalian cells, their hemolytic activity, as well as their mechanism of action. Overall, many of our FLC derivatives exhibited broad-spectrum antifungal activity and all compounds displayed an MIC value of 0.03?μg/mL against at least one of the fungal strains tested. We also found them to be less hemolytic and less cytotoxic to mammalian cells than the FDA approved antifungal agent amphotericin B. Finally, we demonstrated with our best derivative that the mechanism of action of our compounds is the inhibition of the sterol 14α-demethylase enzyme involved in ergosterol biosynthesis.

Synthesis, structure, and biological activity of novel 1H-1,2,4-triazol-1- yl-thiazole derivatives

2-Amino-4-aryl-5-(1H-1,2,4-triazol-1-yl)thiazole derivatives were synthesized from the reaction of α-bromo substituted acetophenone and thiourea. The structures were confirmed by elemental analysis, 1H NMR and single crystal X-ray diffraction analysis. Biological evaluation showed that some of them possess antifungal and plant growth regulatory activities. Copyright Taylor & Francis Group, LLC.