A Novel Approach of Potent Antioxidant and Antimicrobial Agents Containing Coumarin Moiety Accompanied with Cytotoxicity Studies on the Newly Synthesized Derivatives

Abstract

3-Amino-6-(2-oxo-2H-chromen-3-yl)pyridine-2-carbonitrile (2) was synthesized via the reaction of 3-(dimethylamino)acryloyl-2H-chromen-2-one (1) with malononitrile. The reactivity of the 2-amino-3-cyanopyridine derivative 2 toward a variety of electrophiles as triethylorthoformate followed by nitrogenous nucleophiles as hydrazine hydrate was investigated. Also, enamine 1 was utilized as precursor for synthesis of new 3-heteroarylsubstituted coumarins, in which it reacted with a series of hydrazonoyl halides and p-bromobenzenediazonium chloride to yield different3-substituted coumarins. The structures of the newly synthesized derivatives were confirmed by different spectral tools (IR, H 1 NMR, mass spectrometry and elemental analysis). All the newly synthesized compounds were screened for their antioxidant, antimicrobial activities and cytotoxicity. The preliminary structure-activity relationship was discussed to illustrate the essential structure requirements.

Chitosan (CS) / Polyvinyl alcohol (PVA) Films loaded with Novel Synthesized 1,2,3-Triazole Derivative for Cancer Treatment

“…Similarly, compound 5a reacts with 1H-tetrazol-5-amine 12 in ethanol to give tetrazolo [1,5-a] pyrimidine derivative 13 and not 14 (scheme 3). Compound 13 was also well confirmed by IR, 1 HNMR and mass spectral data (see experimental) together with elemental analysis.…”

“…Cancer stands as a leading cause of mortality, responsible for approximately 9 million deaths annually [1][2][3][4] [5]. In the realm of cancer treatment, anticancer agents prove indispensable.…”

Novel Structures of Functionalized Graphene Oxide with Hydrazide: Characterization and Bioevaluation of Antimicrobial and Cytocompatibility Features

“…Using th method, it was observed that after 24 h, the concentrations over 250 µ g/ cells and over 125 µ g/mL for HaCaT cells had a concentration-dependen (Figure 8). Taking into account the general criteria and the conditions rega activity [59], the newly synthesized GOs are fit into the weakly-cyto between 201 and 500 µ g/mL) (Table 4).…”

“…At high concentrations, cell mortality has been increase cells from those that adhered to the surface of the flask were alive and the FDA (Figure 9). Taking into account the general criteria and the conditions regarding a cytotoxic activity [59], the newly synthesized GOs are fit into the weakly-cytotoxic group (IC 50 between 201 and 500 µg/mL) (Table 4). The comparative analysis of the two cell lines reveals a higher cytotoxic effect on HaCaT cells (Figure 8), as also revealed by the lower IC50 for this cell line in comparison with HeLa cells.…”

Investigation of Novel Mucorales Fungal Inhibitors: Synthesis, In‐Silico Study and Anti‐Fungal Potency of Novel Class of Coumarin‐6‐Sulfonamides‐Thiazole and Thiadiazole Hybrids

“…[6] Coumarins, a part of the flavonoid group of plant secondary metabolite, are a wide class of natural and synthetic compounds that showed versatile biological and pharmacological activities. [7][8][9][10][11][12][13][14] Many scientific reports unveiled that natural and synthetic coumarin are drawn considerable attention in medicinal chemistry. [15,16] The great attention paid by researchers to the study of coumarin derivatives is explained by their broad spectrum of biological activities including antiinflammatory, [17] antidiabetic, antiAlzheimer, anticancer, antioxidant, Anticonvulscent, antituberculosis, and as inhibitors of SARS-CoV-2 (COVID-19) virus.…”