Synthesis and Biological Evaluation of Some New Coumarin Derivatives as Antimicrobial Agents

Abstract

The purity of all new compounds was checked by TLC and elucidation of their structures was confirmed by IR, 1 H NMR, and mass spectrometry along with elemental microanalyses. All the target compounds were evaluated for their possible antimicrobial activity. Most of the tested compounds showed weak to moderate antibacterial activity against most of the bacterial strains used in comparison with gatifloxacin as a reference drug. The most active compounds were 6b, 6c, 7b, 8b, 8c, and 9c against B. cereus, E. coli and S. marcescens. Results of antifungal activity revealed that all compounds showed weak to moderate activity against S. brevicaulis, while ketoconazole as a reference drug was completely inactive . Compounds 6a, 6b, 6c, 6e and 7b were even more active than ketoconazole against F. oxysporum.

Coumarin-Based Triapine Derivatives and Their Copper(II) Complexes: Synthesis, Cytotoxicity and mR2 RNR Inhibition Activity

“…IC 50 [µM] a SF c MDA-MB-231 COLO-205 COLO-320 MRC-5 HL 1 4.8 ± 1.3 9.2 ± 0.1 6.7 ± 0.9 41 ± 1 6.1 HL 2 18 ± 4 89 ± 6 83 ± 7 54 ± 5 0.6 HL 3 11 ± 1 76 ± 8 90 ± 10 > 100 1.1 H 2 L 4 3.0 ± 0. Since the antiproliferative activity of TSCs is often related to inhibition of the R2 RNR protein, and may involve the formation of iron complexes of TSCs, first the ability of iron(II) complex with HL 1 to generate ROS was investigated, followed by the potential of selected compounds prepared in this work to reduce the tyrosyl radical in mR2 RNR.…”

“…A series of potentially bidentate (NS), tridentate (ONS or CNS, in particular, for Pd(II) and Ru(II)) Schiff bases is well documented in the literature [40][41][42][43][44][45][46][47][48][49][50]. These have been obtained by condensation reactions of acetyl-, formyl-or trifluoroacetyl-coumarins with substituted thiosemicarbazides.…”

Synthesis, Biological Evaluation and in Silico Adme Predictions of Some New Coumarin-Acetamide Derivatives as Potent Anti-Inflammatory Agents

“…The starting materials 7-hydroxy-4-methyl coumarin 2 21 , ethyl 2-(4-methyl-2-oxo-2Hchromen-7-yloxy) acetate 3 22 , 2-(4-methyl-2oxo-2H-chromen-7-yloxy) acetohydrazide 4 23 were synthesized according to reported procedures.…”

“…The structure of 5 has been also confirmed from EI-MS, the spectrum showed the molecular ion peak M + at m/z 348. 22 IR spectrum of 6 characterized by a broad band at 2700-3600 cm -1 for acidic (OH), and a strong absorption band at 1705 cm -1 corresponding to (C=O) carboxylic.…”