“…When the IR spectrums of compounds are examined, the O-H stretching vibrations of the phenolic -OH group is broad at the range of 3434-3421 cm −1 , and the C=N stretching vibrations of the azomethine group are seen as sharply in the range of 1614-1609 cm −1 . These bands support the completion of the formation reaction of compounds L 1 H-L 3 H. These values agree with those found for similar compounds [14][15][16].…”
Section: Synthesis and Characterization Of The Ligands And Their Cu(i...supporting
confidence: 90%
“…Since sulfonamides are structurally similar to paminobenzoic acid (PABA), a cofactor in folic acid synthesis by bacteria, they can compete with it efficiently to inhibit the synthesis of proteins and nucleic acids, resulting in the inhibition of various microorganisms. Also, it is a sulfonamide, versatile half for its various pharmacological activities, including antibacterial, antifungal, anti-inflammatory, anti-carbonic anhydrase, diuretic, hypoglycemic, antithyroid and antiproton activities, and enzyme inhibition [7][8][9][10][11][12][13][14][15][16]. Sulfonamides, which inhibit the growth of bacterial cells by blocking the synthesis of an important vitamin called folic acid, have also been the subject of many studies due to their significant antitumor activity both in vitro and in vivo [17][18][19][20][21].…”
Synthesis of three Schiff bases of 5-bromo-3-nitro salicylaldehyde containing different sulfonamide group antibiotic compounds and their Cu(II) complexes was carried out. Structures of all compounds were characterized with spectroscopic methods, including Fourier transform infrared, proton nuclear magnetic resonance, and elemental analysis. The in vitro antimicrobial activity of ligands and complexes against Gram-negative and Gram-positive bacteria and the yeast Candida albicans was evaluated. It was determined that the ligand and complexes showed outstanding antimicrobial activity against almost all of the microorganisms tested. It has been observed that the newly synthesized complexes have more antimicrobial effects than the corresponding ligands. It has been determined that the newly synthesized complexes have more antimicrobial effects than the others (E. coli, L. monocytogenes, and C. albicans), especially on Staphylococcus aureus and Pseudomonas aeruginosa.
“…When the IR spectrums of compounds are examined, the O-H stretching vibrations of the phenolic -OH group is broad at the range of 3434-3421 cm −1 , and the C=N stretching vibrations of the azomethine group are seen as sharply in the range of 1614-1609 cm −1 . These bands support the completion of the formation reaction of compounds L 1 H-L 3 H. These values agree with those found for similar compounds [14][15][16].…”
Section: Synthesis and Characterization Of The Ligands And Their Cu(i...supporting
confidence: 90%
“…Since sulfonamides are structurally similar to paminobenzoic acid (PABA), a cofactor in folic acid synthesis by bacteria, they can compete with it efficiently to inhibit the synthesis of proteins and nucleic acids, resulting in the inhibition of various microorganisms. Also, it is a sulfonamide, versatile half for its various pharmacological activities, including antibacterial, antifungal, anti-inflammatory, anti-carbonic anhydrase, diuretic, hypoglycemic, antithyroid and antiproton activities, and enzyme inhibition [7][8][9][10][11][12][13][14][15][16]. Sulfonamides, which inhibit the growth of bacterial cells by blocking the synthesis of an important vitamin called folic acid, have also been the subject of many studies due to their significant antitumor activity both in vitro and in vivo [17][18][19][20][21].…”
Synthesis of three Schiff bases of 5-bromo-3-nitro salicylaldehyde containing different sulfonamide group antibiotic compounds and their Cu(II) complexes was carried out. Structures of all compounds were characterized with spectroscopic methods, including Fourier transform infrared, proton nuclear magnetic resonance, and elemental analysis. The in vitro antimicrobial activity of ligands and complexes against Gram-negative and Gram-positive bacteria and the yeast Candida albicans was evaluated. It was determined that the ligand and complexes showed outstanding antimicrobial activity against almost all of the microorganisms tested. It has been observed that the newly synthesized complexes have more antimicrobial effects than the corresponding ligands. It has been determined that the newly synthesized complexes have more antimicrobial effects than the others (E. coli, L. monocytogenes, and C. albicans), especially on Staphylococcus aureus and Pseudomonas aeruginosa.
“…A series of coumarin-sulfonamide hybrids was synthesized by the condensation reaction of appropriate N -heteroaryl-4-amino benzenesulfonamide with derivatives of 3-acetyl coumarin and their antiproliferative property was screened against the MDA-MB-231, MIA PaCa-2, and H357 cancer cell lines. 182 Among them, compound 112 ( Fig. 110 ) demonstrated significant activity against the MDA-MB-231 cell line (IC 50 = 7.78 ± 3.78 μM) and H357 cell line (IC 50 = 8.68 ± 1.10 μM) after 72 h.…”
Many researchers all around the world are working on the development of novel anticancer drugs with different mechanisms of action. Coumarin is a highly promising pharmacophore for the development of...
“…Moreover, Chromene derivatives are an essential class of oxygen-containing heterocyclic compounds that have attracted researcher's attention because of their applications in pigments, cosmetics, and agrochemicals, and their wide range of biological activities 17 , 18 like anti-diabetic 19 , antibacterial 20 , antioxidant 21 , anti-cancer 22 and antiviral activities 23 . Given that chromene sulfonamide hybrids have been shown variable biological activities 24 – 26 , and based on our previous works on the synthesis of sulfonamide hybrids 27 – 31 , accordingly, we were motivated to design and synthesize some novel derivatives of these hybrids (Scheme 1 ). Scheme 1 Synthesis of novel chromene-sulfonamide hybrids.…”
In this study, eleven novel chromene sulfonamide hybrids were synthesized by a convenient method in accordance with green chemistry. At first, chromene derivatives (1–9a) were prepared through the multi-component reaction between aryl aldehydes, malononitrile, and 3-aminophenol. Then, synthesized chromenes were reacted with appropriate sulfonyl chlorides by grinding method to give the corresponding chromene sulfonamide hybrids (1–11b). Synthesized hybrids were obtained in good to high yield and characterized by IR, 1HNMR, 13CNMR, CHN and melting point techniques. In addition, the broth microdilution assay was used to determine the minimal inhibitory concentration of newly synthesized chromene-sulfonamide hybrids. The MTT test was used to determine the cytotoxicity and apoptotic activity of the newly synthesized compounds against fibroblast L929 cells. The 3D‑QSAR analysis confirmed the experimental assays, demonstrating that our predictive model is useful for developing new antibacterial inhibitors. Consequently, molecular docking studies were performed to validate the findings of the 3D-QSAR analysis, confirming the potential binding interactions of the synthesized chromene-sulfonamide hybrids with the target enzymes. Molecular docking studies were employed to support the 3D-QSAR predictions, providing insights into the binding interactions between the newly synthesized chromene-sulfonamide hybrids and their target bacterial enzymes, thereby reinforcing the potential efficacy of these compounds as antibacterial agents. Also, some of the experimental outcomes supported or conflicted with the pharmacokinetic prediction (especially about compound carcinogenicity). The performance of ADMET predictor results was assessed. The work presented here proposes a computationally driven strategy for designing and discovering a new sulfonamide scaffold for bacterial inhibition.
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