A new series of cyclic coumarin-fluorocytosine hybrid conjugates (N1-N6) was synthesized through microwave technology. The synthetic plan involved the formation of the required Schiff base N, followed by the transformation of the azomethine functional group of the Schiff base N to oxazepine and imidazolidone rings. The antimicrobial activity of the synthesized compounds N-N6 was assessed against Gram-positive bacteria (Staphylococcus aureus and Staphylococcus epidermidis) and Gram-negative bacteria (Escherichia coli, Pseudomonas, and Klebsiella) using the disk diffusion method. Compounds N4 and N5 showed the highest activity against S. aureus (24 mm inhibition), with N5 also demonstrating superior inhibition against Klebsiella and Pseudomonas. Molecular docking studies with DNA gyrase enzymes (Protein Data Bank: 1AJ6 for (E. coli) and 3G7B for (S. aureus) revealed that compound N5 strongly binds to both (E. coli) (–9.28 kcal/mol) and (S. aureus) (–9.65 kcal/mol), involving hydrogen bonds, hydrophobic interactions, and halogenation at conserved active site residues. All compounds met Lipinski's criteria, did not cross the blood-brain barrier, and displayed favorable gastrointestinal absorption and bioavailability according to absorption, distribution, metabolism, and excretion predictions. Overall, these hybrid compounds, especially N5, show promise as antimicrobial agents.. KEYWORDS :Coumarin, Fluorocytosine, Cycloaddition, Molecular docking.
The present report depicts a convenient route for the synthesis of new N-Mannich bases from Ciprofloxacin (CP) drug. The synthetic route started from the reaction CP drug with 2-mercaptobenzimidazole to give compound [A], the N-Mannich bases analogs of CP [A1-A8] were prepared by the reaction of CP derivative [A] with primary and secondary amine derivatives. The structure of the analogs was confirmed by spectral (1 HNMR and FTIR) and analytical data. This study also includes calculations of total energy and electrostatic potential. In addition, this research aimed to determine the effects of CP derivatives on the activity of various transferase enzymes in sera, such as serum glutamic-oxaloacetic transaminase (GOT) and Glutamate Pyruvate Tra
... Show MoreA new methodology was applied to the synthesis of new imidazolones and oxyazepine derivatives containing imidazo thiazole fused rings. Starting with 5-(4-bromo phenyl) imidazo (2, 1-b) thiazole, which was synthesized using the standard procedure, the Carbaldehyed group was introduced at position 6 of 5-(4-bromo phenyl) imidazo (2, 1-b) thiazole. Then, this 6-carbaldehyed derivative was condensed with different substituted aromatic amines to afford new Schiff bases. The latter were cyclized into new oxazepine and imidazolone derivatives by using phthalic anhydride and glycine, respectively. These new derivatives were characterized by using FT-IR, 1HHNMR, and 13CNMR spectra, as well as examined (evaluated) for anti-bacterial and anti-fungal a
... Show MoreNew series of Schiff bases 2(a-j) and corresponding beta-lactam derivatives 3(a-j) were synthesized from cefalexin (1) as starting material. The compound (1) was reacted with different aldehydes and ketones to give Schiff bases derivatives 2(a-j). The synthesized Schiff bases were cyclized by chloroacetyl chloride in the presence of triethylamine to form beta-lactam derivatives 3(a-j). The compounds were characterized by deremination melting point, FT-IR and 1H NMR. The beta-lactam derivatives were screened in vitro antibacterial against some bacterial species
New derivatives of pyromellitamic diacids and pyromellitdiimides have been prepared by the reaction of one mole of pyromellitic dianhydride with two moles of aromatic amines, these derivatives were characterized by elemental analysis, FT-IR and melting point.
Background: Green Tea is made from the leaf of the plant “Camellia sinensisâ€. Green tea is reported to contain thousands of bioactive ingredients including catechins which have shown great promise for having antimicrobial effects. Periodontal diseases represent one of the most prevalent diseases around the world and the main etiologic factor behind it, is plaque accumulation, in addition certain kinds of bacteria have been detected frequently in subjects suffering from periodontitis, Several studies suggested that the outcome of periodontal treatment is better if particular pathogens including Aggregatibacteractinomycetemcomitans can no longer be detected after therapy. Materials and Methods: plaque samples were collected from 2
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