Ultrasound-Promoted Synthesis of Biologically Active α-Hydroxyphosphonates/ Hydroxyphosphinates Using 1,4-Dimethylpiperazine as a Catalyst

<div><p> </p><p>A series of new α-hydroxyphosphonates/phosphinates was prepared using 1,4-dimethylpiperazine as a base catalyst under conventional as well as ultrasonic irradiation conditions by the reaction of 5-bromoindole-3-carboxaldehyde/2-nitrocinnamaldehyde with various phosphonates/phosphinates. The high yields of α-hydroxyphosphonates/hydroxyphosphinates were obtained in less reaction time under the ultrasonic irradiation method as compared with the conventional method. The synthesized compounds were screened for their in vitro and in vivo antioxidant activities, and the bio-screening data revealed that all the tested compounds exhibited good antioxidant activities. The bio-screening data revealed that compound <b>8e</b> exhibited potent antioxidant activity in both in vitro and in vivo studies while the other compounds exhibited good antioxidant activity.</p><p>[Supplementary materials are available for this article. Go to the publisher's online edition of <i>Phosphorus, Sulfur, and Silicon and the Related Elements</i> for the following free supplemental files: Additional text, tables and figures.]</p></div

Synthesis Of New P-substituted Iminophosphoranes Via Staudinger Raction And Antimicrobial Activity Evaluation

<p>A class of two series of new P-substituted iminophosphoranes, N-(1,3-benzothiazol-2-ylmethyl)-N-(alkyl subtituted-λ⁵-phosphanylidene)amine <b>5(a-e)</b> and N-(alkyl substituted-λ⁵-phosphanylidene)-(3,5-difluorophenyl)methanamine <b>9(a-e)</b> was accomplished via Staudinger reaction of sodium azide, 2-chloromethyl benzothiazole <b>(1)</b> or 3,5-difluorobenzylbromide <b>(6)</b> and various trivalent alkyl/aryl phosphines/ethyldiphenylphosphinite/dimethylphenylphosphonite <b>4(a-e)</b>. The structures of new products were elucidated from spectroscopic data and elemental analysis. In vitro antibacterial and antifungal activities of the title compounds were investigated against four bacterial strains and three fungal strains at 50 and 100 μg/mL concentrations, respectively. The minimum inhibitory concentration (MIC) of the title compounds were also determined. Among all the compounds, 3,5-difluorobenzyl core derivatives <b>9a</b> and <b>9b</b>, and 1,3-benzothiazol-2-ylmethyl constituent containing compounds, <b>5b</b> and <b>5c</b> showed promising antibacterial and antifungal activities, respectively, at lower MIC values in the range of 6.25–25.0 μg/mL and approximately closer to the standards.</p

Bismuth(III) Chloride Mediated Michaelis–Arbuzov Reaction: A Facile Synthesis of Substituted Arylphosphonates/Phosphinates and Bioactivity Evaluation

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

Synthesis of Novel <i>N,N</i>-Disubstituted Ethyl <i>P</i>-[2-(1<i>H</i>-Indol-3-YL)Acetyl]Phosphoramidates and Their Biological Activity

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

Synthesis, spectral characterization and bioactivity evaluation of novel α-aminophosphonates

<p>A facile synthesis of novel α-aminophosphonates <b>5a-j</b> was accomplished by condensation of imines (<b>3a-j)</b> with diethyl phosphite (<b>4</b>) in ethanol at 50–60°C using easily recoverable and reusable catalyst, tetramethyl guanidine (TMG) via pudovik reaction in high yields. All the title compounds were characterized by spectral and elemental analysis. They were further screened for their abilities towards <i>in vitro</i> antibacterial, antifungal and antioxidant activities. The compounds <b>5g</b>, <b>5d, 5f</b> exhibited good antibacterial and antifungal activities compared to the standard bactericide, Penicillin and fungicide, Griseofulvin, respectively. The compounds <b>5h</b>, <b>5i</b>, <b>5g</b>, and <b>5c</b> exhibited good antioxidant activity compared to the standard ascorbic acid.</p