Synthesis and characterization of oxazine bearing pyridine scaffold as potential antimicrobial agents

<p>A series of novel compounds 1-((1-(4-(2<i>H</i>-benzo[e][1,3]oxazin-3(4<i>H</i>)-yl)phenyl)ethylidene)amino)-6-((benzylidene)amino)-2-oxo-4-phenyl-1,2-dihydropyridine-3,5-dicarbonitriles <b>(7a–o)</b> were synthesized by a sequence of multistep reactions. IR, ¹H NMR, ¹³C NMR, and mass spectral techniques were used to confirm the structures newly synthesized compounds. Antimicrobial activity of the title compounds <b>(7a–o)</b> was studied against strains of bacteria (<i>Staphylococcus aureus</i> and <i>Streptococcus pyogenes, Escherichia coli</i> and <i>Pseudomonas aeruginosa</i>) and fungi (<i>Candida albicans, Aspergillus niger</i> and <i>Aspergillus clavatus</i>) by serial dilution method. Compounds <b>7f</b> and <b>7k</b> exhibited significant antimicrobial activity.</p

Studies on Antimicrobial Evaluation of Some 1-((1-(1<i>H</i>-Benzo[<i>d</i>]imidazol-2-yl)ethylidene)amino)-6-((arylidene)amino)-2-oxo-4-phenyl-1,2-dihydropyridine-3,5-dicarbonitriles

<div><p></p><p>A new series of 1-((1-(1<i>H</i>-benzo[<i>d</i>]imidazol-2-yl)ethylidene)amino)-6-((arylidene)amino)-2-oxo-4-phenyl-1,2-dihydropyridine-3,5-dicarbonitriles <b>(4a–o)</b> have been synthesized for the development of antimicrobial agents. Newly synthesized compounds were evaluated for their in vitro antibacterial activity against Gram-positive bacteria (<i>Pseudomonas aeruginosa</i>, <i>Streptococcus pyogenes</i>), Gram-negative bacteria (<i>Escherichia coli</i>, <i>Staphylococcus aureus</i>), and antifungal activity (<i>Candida albicans</i>, <i>Aspergillus niger</i>, <i>Aspergillus clavatus</i>). These compounds were characterized by infrared, ¹H NMR, ¹³C NMR, and mass spectra. The synthesized compounds <b>4b, 4e, 4 h,</b> and <b>4k</b> showed potent antimicrobial activity against tested microorganisms.</p></div

Synthesis, biological evaluation, and molecular docking study of pyridine clubbed 1,3,4-oxadiazoles as potential antituberculars

<p>A series of pyridine clubbed 1,3,4-oxadiazole derivatives were efficiently synthesized, characterized by standard spectral techniques and evaluated for their <i>in vitro</i> antitubercular activity against <i>Mycobacterium tuberculosis</i> (MTB) H₃₇Ra and <i>Mycobacterium bovis</i> BCG in active and dormant state using an established methods. Compounds <b>5a, 5m</b>, and <b>5t</b> were identified as the most active compounds against MTB. Molecular docking was performed against MTB enoyl-ACP (CoA) reductase (FabI/ENR/InhA) enzyme to predict the binding modes and affinity. The theoretical predictions from molecular docking could establish a link between the observed biological activity and the binding affinity shedding light into specific bonded and non-bonded interactions influencing the activity. The active compounds were studied for cytotoxicity against three cell lines and were found to be non-cytotoxic. Specificity of these compounds was checked by screening them for their antibacterial activity against four bacterial strains.</p