Résumé: A computational Petra/Osiris/Molinspiration/DFT (POM/DFT) based model has been developed for the identification of physico-chemical parameters governing the bioactivity of series of oxazaphosphinanes derivatives 1a-1f containing potential antifungal O, N-pharmacophore. Molecular docking study was performed in order to evaluate synthesized compounds their possible antifungal properties and their interactions in the binding site. Molecular docking studies revealed that the compounds 1a-1f have the potential to become lead molecules in the drug discovery process. The six compounds 1a–1f analyzed here were previously synthesized by our group.

Résumé: A series of novel α-sulfamidophosphonate derivatives was rationally designed and synthesized following the principle of the superposition of bioactive substructures by the combination of sulfonamide, aldehyde and triethylphosphite. The relative cytotoxicity of these derivatives in comparison to chlorambucil has been reported. The crystal structure of diethyl phenyl (N-phenylsulfamoylamino)methylphosphonate has been determined. This crystal belongs to the C 2/c space group. The P atom has a distorted tetrahedral configuration with the O-P-O angle as the minimum bond angle (105.34) and one of the O=P-O angles as the maximum angle (116.18). In addition, the results of bioinformatics POM analyses and molecular docking show that all compounds exhibited good bioavailability, pharmacokinetic, and no toxicity profiles. Furthermore, drug likeness analysis suggests that the synthesized αsulfamidophosphonate derivatives might have appropriate oral absorption and brain penetration for therapeutic applications. As the compounds were found to be non-toxic and in a safe range containing an important antiviral O,O-pharmacophore site, they present good candidates for further antiviral study.

Résumé: Some novel N-sulfonylphthalimides were synthesized in good yields by condensation of anhydride phthalic with various sulfonamides by two different methods: conventional synthesis and immersion ultrasonic assisted method, in one step. These compounds were screened for their antibacterial activity against Escherichia coli, Staphylococcus aureus, Morganella morganii and Klebsiella pneumoniae.The bioinformatic POM analyses confirm the existence of a antifungal/or antiviral (O d- ——O d- ) pharmacophore sites. So it will benificial to test these molecules against other biotargets different of bacterial strains such as viruses, fungus and parasites.The molecular structure of 3a was obtained by X-ray diffraction on mono crystal. The crystal packing can be described as alternating layers in zigzag parallel to (100) plane along the c axis, which are connected together with CeH/O hydrogen bonds.

Résumé: An easy and handy synthesis of α-sulfamidophosphonates directly by Three-Component reactions is reported. The reaction involves the use of aldehyde, sulfonamides and trimethylphosphite. A wide range of substrates is compatible in this reaction, producing excellent yields in short time. The reaction is performed under solvent-and catalyst-free conditions using microwave irradiation, greener conditions and lower generation of waste or pollution are the main advantages of this method.

Résumé: Several new sulfamidocarbonyloxyphosphonates were prepared in two steps, namely carbamoylation and sulfamoylation, by using chlorosulfonyl isocyanate (CSI), α-hydroxyphosphonates, and various amino derivatives and related (primary or secondary amines, β-amino esters, and oxazolidin-2-ones). All structures were confirmed by 1 H, 13 C, and 31 P NMR spectroscopy, IR spectroscopy, and mass spectroscopy, as well as elemental analysis. Eight compounds were evaluated for their in vitro antibacterial activity against four reference bacteria including Gram-positive Staphylococcus aureus (ATCC 25923), and Gram-negative Escherichia coli (ATCC 25922), Klebsiella pneumonia (ATCC 700603), Pseudomonas aeruginosa (ATCC 27853), in addition to three clinical strains of each studied bacterial species. Compounds 1a–7a and 1b showed significant antibacterial activity compared to sulfamethoxazole/trimethoprim, the reference drug used in this study.

Résumé: A facile and versatile method for acylation of structurally diverse amines and sulfonamides under focused ultrasonic irradiation in catalyst-free and solvent-free conditions is reported. There are several advantages to this approach such as simple and easier workup conditions, small amount of time and high yielding. The acylation reaction was carried out with acetic anhydride. All structures of synthesized products have been identified by NMR and mass spectroscopy.

Résumé: An improved environmentally benign method for synthesis of sulfamides under focused ultrasound irradiation and under solvent-free and catalyst-free conditions has been carried out by the reaction of amines or amino esters with sulfuryl chloride. This approach allows the synthesis of products in excellent yields and in short reaction time.

Résumé: In this paper, the structural analysis of two novel derivatives of N-Acylsulfonamides (1a-1b) has been made. Packings of the two crystal structures presented herein are the results of individually weak but synergistic non covalent interactions like typical NH... O=(C or S) hydrogen bonds or π/π stacking effects. DFT calculation of molecular electrostatic potentials

Résumé: Correction for ‘A novel, rapid and green method of phosphorylation under ultrasound irradiation and catalyst free conditions’ by Abdeslem Bouzina et al., RSC Adv., 2015, 5, 46272–46275.

Résumé: A convenient method for the synthesis of new series of N-acylsulfonamide containing oxazolidin-2-one moiety starting from chlorosulfonyl isocyanate and chiral oxazolidinones in two steps (carbamoylation and sulfamoylation), is described. The starting oxazolidinones were obtained in two steps starting from amino acids by reduction with NaBH4 then cyclization in the presence of carbonate diethyl. The synthesis of N-acylsulfonamide oxazolidin-2-ones derivatives has been carried out in excellent isolated yields. The structures of all synthesized compounds were unambiguously confirmed by usual spectroscopic methods 1H NMR, 13C NMR, IR, EA and MS.

Résumé: A new series of N,N-bis-oxazolidinones-sulfone and 5-chloromethylsulfamoyl-oxazolidin-2-ones have been synthesized in three steps (carbamoylation, sulfamoylation and cyclization) starting from 1,3-dichloroporopan-2-ol, chlorosulfonyl isocyanate and primary or secondary amines. Synthesis has been carried out following simple methodology in excellent isolated yields. The structure and purity of the original compounds were confirmed by IR, NMR, and MS. The compounds were evaluated for their in vitro antibacterial activity against some Gram-positive bacteria; Staphylococcus aureus and Gram-negative bacteria; Escherichia Coli, Klebsiella pneumonieae, Acinetobacter, Pseudomonas aeruginosa, Enterococcus, Salmonella sp. The compounds showed moderate to good antibacterial activity.

Résumé: A new series of sulfonylcycloureas derivatives have been synthesized and evaluated in vitro for their antitumor activity against four cancer cell lines (A431, Jurkat, U266, and K562). These compounds were prepared by the condensation of several sulfonamides (2a–m) with ethyl bis(2-chloroethyl)carbamate (1a). The relative cytotoxicity of these new derivatives in comparison to chlorambucil is reported.

Résumé: An efficient and convenient one-pot synthesis of novel α-sulfamidophosphonates is described via a three-component reaction. This reaction was carried out through a three component condensation reaction of sulfonamide, an aromatic aldehyde and triethylphosphite under conventional/ultrasonic techniques, catalyst-free and solvent-free conditions. This methodology was established with many advantages, including mild reaction conditions, short reaction times, good yields, simple work-up procedures, and environmental friendliness.

Résumé: The phosphorylation reaction of various N-acylamines, N-acylaminoesters N-acylaminoalcohols and N-acylsulfonamides with trimethylphosphite or triethylphosphite was effectively promoted under ultrasound irradiation, solvent and catalyst free conditions to produce the corresponding amidophosponate. This rapid method produced the products in short reaction times (5–15 min) and excellent yields (75–90%). This technique at a frequency of 40 kHz, strongly accelerates the process of formation of P–C bonds compared to the classic Arbuzov reaction.

Résumé: A rapid and efficient solvent-free one-pot synthesis of novel oxazaphosphinane is described under ultrasound irradiation. This reaction was carried out through a three-component condensation reaction of amino alcohol, aromatic aldehyde, and triethyl phosphite. Ultrasonic effects were established with many advantages, including high yields, shorter reaction times, easy and quick isolation of the products. The newly synthesized compounds were systematically characterized by IR, 1H NMR, 13C NMR, 31P NMR, MS, and elemental analysis.

Résumé: The oxazolidin-2-ones are key intermediates in the synthesis of various compounds of interest in terms of reactivity. So, several aminoalcohols were prepared from oxazolidinone. The oxazolidinone may also be used as an intermediate in the preparation of peptidosulfonamide similar sulfonated a natural or synthetic peptide. The reactive condition typical for conversion of the cycle oxazolidinone from the aminoalcohol involves the use of a base hydroxyl, water and different types of organics co-solvents.

Résumé: The condensation of various sulfonamides with aromatic aldehydes was effectively promoted in the presence of TBAB to produce the corresponding sulfonylimine products in good yields under solvent-free conditions. The sulfonamides were prepared starting from chlorosulfonylisocyanate (CSI), primary amine in three steps (carbamoylation, sulfamoylation and deprotection).