Synthesis of Novel 1,2,3-Triazole-dihydro[3,2-<i>c</i>]chromenones as Acetylcholinesterase Inhibitors

<div><p></p><p>A novel series of 1,2,3-triazole-dihydro[3,2-c]chromenone derivatives were synthesized through an efficient three-step reaction starting from 4-hydroxybenzaldehyde. All the newly synthesized compounds were characterized by infrared and NMR spectroscopy as well as elemental analysis and evaluated for their acetylcholinesterase inhibitory activity.</p></div

Vilsmeier Reagent: An Efficient Reagent for the Transformation of 2-Aminobenzamides into Quinazolin-4(3<i>H</i>)-one Derivatives

<div><p></p><p>Clean and easy preparation of quinazolin-4(3H)-one derivatives using 2-aminobenzamides and Vilsmeier reagent is described. 2-Aminobenzamides were converted into the corresponding quinazolinones under mild and efficient conditions, in good yields without undesirable by-products.</p> <p>[Supplementary materials are available for this article. Go to the publisher's online edition of <i>Synthetic Communications</i>® for the following free supplemental resource(s): Full experimental and spectral details.]</p> </div

Quinoline-based imidazole-fused heterocycles as new inhibitors of 15-lipoxygenase

<p>A series of 2-chloro-quinoline-based imidazopyridines <b>6a–l</b> and imidazothiazoles <b>6m–o</b> bearing a bulky alkylamine side chain were synthesized as soybean 15-LOX inhibitors. The target compounds <b>6a–o</b> were prepared <i>via</i> one-pot reaction of 2-chloroquinoline-3-carbaldehyde (<b>3</b>), heteroaromatic amidine <b>4</b>, and alkyl isocyanides <b>5</b>, in the presence of NH₄Cl. All compounds showed significant anti-15-LOX activity (IC₅₀ values ≤40 μM). Among the title compounds, the imidazo[2,1-<i>b</i>]thiazole derivative <b>6n</b> bearing a <i>tert</i>-butylamine moiety showed the highest activity against soybean 15-LOX enzyme.</p

Efficient three-step synthesis of benzo[<i>e</i>]imidazo[1,2-<i>c</i>][1,2,3]triazines

<p>A novel three-step sequence toward benzo[<i>e</i>]imidazo[1,2-<i>c</i>][1,2,3]triazine derivatives is investigated. This pathway started from commercially available starting materials afforded <b>5a–h</b> in good to excellent yields. In this method, we took the advantage of diazonium chemistry, which was followed by intramolecular N-N bond formation in the construction of N-rich cycles.</p

An efficient, four-component reaction for the synthesis of novel carbamodithioates

<p>A series of substituted phenylcarbamoyl methyl benzylcarbamodithioates have been synthesized using the multicomponent condition. The reaction proceeded under mild practical condition and afforded the desired products in good yields.</p

Straightforward Approach Toward Dihydrothiazoles via Intramolecular Bromocyclization

<div><p></p><p>An intramolecular bromonium ion–assisted cyclization with sulfur as an internal nucleophile is described. Starting from benzoyl chlorides, this method provides an easy procedure for the synthesis of dihydrothiazole derivatives in moderate to good yields.</p></div

Synthesis of Novel 4<i>H</i>-Chromenes Containing a Pyrimidine-2-Thione Function in the Presence of Fe₃O₄ Magnetic Nanoparticles and Study of Their Antioxidant Activity

<div><p>GRAPHICAL ABSTRACT</p><p></p></div

Synthesis and Evaluation of Coumarin–Resveratrol Hybrids as 15-Lipoxygenaze Inhibitors

<div><p></p><p>A series of coumarin–resveratrol hybrids, 3-arylcoumarin derivatives <b>3a–u</b>, were synthesized through the intermolecular condensation reaction of various salicylaldehydes and phenylacetic acids in the presence of 1,4-diazabicyclo[2.2.2]octane under solvent-free conditions. All the synthesized compounds were screened for their inhibitory potency against soybean 15-lipoxygenase. Among them, three compounds (<b>3c</b>, <b>3j</b>, and <b>3q</b>) showed good enzyme-inhibitory activities.</p></div