Synthesis of novel sulfonamide analogs containing sulfamerazine/sulfaguanidine and their biological activities

<p>Sulfamerazine and sulfaguanidine are clenched with <i>p</i>-nitrobenzoyl chloride and the products obtained are reduced to Na_xS in ethanol–water. Novel sulfonamides (<b>6a</b>–<b>g</b> and <b>9a</b>–<b>g</b>) were synthesized by the reaction of these reduced products (<b>4</b> and <b>8</b>) with various sulfonyl chlorides (<b>5a</b>–<b>g</b>). The structures of these compounds were characterized using spectroscopic analysis (IR, ¹H-NMR, ¹³C-NMR and HRMS) technique. Antimicrobial activity of sulfonamides (<b>3, 4, 7, 8, 6a–g</b> and <b>9a</b>–<b>g</b>) was evaluated by the agar diffusion method. These compounds showed antimicrobial activity against tested microorganism strains (Gram-positive bacteria, clinic isolate and yeast and mold). Compounds <b>9d</b>, <b>9e</b>, <b>9a</b>, <b>6d</b> and <b>6e</b> showed particularly antimicrobial activity against tested Gram-positive (<i>Bacillus cereus</i> and <i>B. subtilis</i>) and Gram-negative (<i>Enterobacter aerogenes</i>) bacteria.</p

One-Pot, Facile, Highly Efficient, and Green Synthesis of Acridinedione Derivatives Using Vitamin B₁

<div><p></p><p>An efficient methodology for the synthesis of acridinedione derivatives <b>4a-o</b> has been achieved by one-pot, multi-component condensation of dimedone <b>1</b>, various amines <b>2a-d</b> and substitute aromatic aldehydes <b>3a-k,</b> in the presence of the easily available, inexpensive, and nontoxic catalyst vitamin B₁ (<b>VB</b>_<b>1</b>) as a versatile biodegradable. Synthesis of acridine-type compounds was performed in high yields in water as green solvent. Its high-yield efficiency, clean, eco-friendly, simple work-up procedure, and easy purification are regarded to be the main advantages of this method besides its being green solvent. The synthesized compounds are characterized using spectroscopic analyses (IR, ¹H-NMR, ¹³C-NMR and HRMS) techniques.</p></div