147715-84-2Relevant academic research and scientific papers
Convenient Synthesis of Novel N -Acylsulfonamides Containing Phosphonate Moiety
Boufas, Wahida,Cheloufi, Hadjer,Bouchareb, Fouzia,Berredjem, Malika,Aouf, Nour-Eddine
, p. 103 - 111 (2015/10/29)
The present study describes a convenient method for the synthesis of new N-acylsulfonamides containing phosphonate moiety. The N-acylsulfonamides were prepared starting from chlorosulfonyl isocyanate (CSI) in four steps (carbamoylation, sulfamoylation, deprotection, and acylation). Trimethylphosphite has been used to introduce the phosphonate moiety into N-acylsulfonamides via Arbuzov reaction. GRAPHICAL ABSTRACT
An efficient method for the synthesis of novel n-acylsulfonamides using tin (IV) chloride as catalysts
Bouchareb, Fouzia,Boufas, Wahida,Cheloufi, Hadjer,Berredjem, Malika,Aouf, Nour-Eddine
, p. 587 - 595 (2014/06/09)
A series of novel N-acylsulfonamides derivatives were synthesized via direct condensation of parent sulfonamide with ethyl lactate as an acylating agent in the presence of tin (IV) chloride (SnCl4) as a Lewis acid catalyst. The sulfonamides were prepared, starting from chlorosulfonyl isocyanate (CSI), in three steps (carbamoylation, sulfamoylation, and deprotection) with excellent yields. Copyright
Synthesis and antibacterial activity of sulfonamides. SAR and DFT studies
Boufas, Wahida,Dupont, Nathalie,Berredjem, Malika,Berrezag, Kamel,Becheker, Imène,Berredjem, Hajira,Aouf, Nour-Eddine
, p. 180 - 185 (2014/07/08)
A series of substituted sulfonamide derivatives were synthesized from chlorosulfonyl isocyanate (CSI) in tree steps (carbamoylation, sulfamoylation and deprotection). Antibacterial activity in vitro of some newly formed compounds investigated against clinical strains Gram-positive and Gram-negative: Escherichia coli and Staphylococcus aureus applying the method of dilution and minimal inhibition concentration (MIC) methods. These compounds have significant bacteriostatic activity with totalities of bacterial strains used. DFT calculations with B3LYP/6-31G(d) level have been used to analyze the electronic and geometric characteristics deduced for the stable structure of three compounds presenting conjugation between a nitrogen atom N through its lone pair and an aromatic ring next to it. The principal quantum chemical descriptors have been correlated with the antibacterial activity.
Carbonic anhydrase inhibitors: Inhibition of cytosolic isozymes I and II with sulfamide derivatives
Casini, Angela,Winum, Jean-Yves,Montero, Jean-Louis,Scozzafava, Andrea,Supuran, Claudiu T.
, p. 837 - 840 (2007/10/03)
A novel class of effective CAIs has been identified, starting from a very weak carbonic anhydrase inhibitor (CAI), sulfamide, whose X-ray crystal structure in the adduct with hCA II has recently been reported. A series of N,N-disubstituted- and N-substitu
A new family of potential oncostatics: 2-Chloroethylnitrososulfamides (CENS) - I. Synthesis, structure, and pharmacological evaluation (preliminary results)
Abdaoui, Mohamed,Dewynter, Georges,Aouf, Nourredine,Favre, Gilles,Morere, Alain,Montero, Jean-Louis
, p. 1227 - 1235 (2007/10/03)
A new series of alkylating agents, 2-chloroethylnitrososulfamides (CENS), were developed on the model of 2-chloroethylnitrosoureas. Starting from chlorosulfonyl isocyanate, a four-step synthesis (carbamoylation-sulfamoylation, Mitsunobu alkylation, deprotection, and nitrosation) gives the title compounds in a 47-58% overall yield. The selection of the nitrosation site can be directed through an alternative route. The pharmacological evaluation shows a significant oncostatic activity towards both A549 and MCF7 cell lines.
