Design, synthesis and evaluation of novel quinazoline-2,4-dione derivatives as chitin synthase inhibitors and antifungal agents

Synthesis and biological evaluation of novel 3-substituted amino-4-hydroxylcoumarin derivatives as chitin synthase inhibitors and antifungal agents

“…The stock solutions of the candidate compounds were made by dissolving compounds with DMSO for no more than 10.0 g/L and diluting with sterile water for final concertration of DMSO below 3%. The solution of the candidate compounds was made by diluting the stock solution with 50 mM Tris-HCl buffer solution at pH 7.5 36,37 . Two hundred microliters 30 lg/mL wheatgerm agglutinin (WGA) stock solutions in 50 mmol/L Tris-HCl at pH 7.5 were added to each well of the microplate and were incubated at room temperature for 16 h, then the solutions in the wells were removed and the plates were washed at least three times with distilled water.…”

“…In continuation of previous study for developing new CHS inhibitors 37 , in this work we focused our attention on 3-substituted amino-4-hydroxycoumarin derivatives bearing an N-phenylpiperazine group on L-tartaric amide side chain. We expected that substituting the 3-position of the coumarin with a linear moiety which resembles roughly the side chain of polyoxins B and Nikkomycin Z (Figure 3) would lead to novel derivatives of coumarin which possess broad-spectrum antifungal activity and CHS inhibition activity.…”

Gadolinium(III)‐Based Dual 1H/19F Magnetic Resonance Imaging Probes

“…The ligands H 3 L 1 and H 2 L 2 were synthesized by alkylations of the tris‐ or bis‐protected cyclen derivatives DO3A t Bu or DO2A t Bu, respectively, with chloromethyl acetamides 1 a and 1 b (Scheme ). These precursors were prepared in one step by reactions of chloroacetyl chloride with the respective fluorinated anilines . The ligands were isolated in near‐quantitative overall yields (>98 %) following removal of the tert ‐butyl protecting groups with formic acid.…”

Ionic liquid catalysed multicomponent synthesis, antifungal activity, docking studies and in silico ADMET properties of novel fused Chromeno-Pyrazolo-Phthalazine derivatives

“…All synthesized compounds were dissolved in DMSO as stoke solutions. The antifungal activity was evaluated by disc diffusion method, [28]. The inhibition action was tested after incubating for 48 h at 37 °C and the minimum inhibitory concentrations (MICs, mg/mL) were recorded.…”