3984-18-7Relevant 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.
Macrocyclic compounds as inhibitors of viral replication
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, (2008/06/13)
The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
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
Basicity of Nitrogen-Sulphur(VI) Compounds. Part 6. Ionization of NN'-Di- and N-Mono-substituted Sulphamides and Dihydro-2,1,3-benzothiadiazoline and Benzothiadiazine 2,2-Dioxides (Cyclic Sulphamides)
Burke, Padraig O.,McDermott, Sean D.,Hannigan, Thomas J.,Spillane, William J.
, p. 1851 - 1854 (2007/10/02)
36 Di- and mono- and two tri-substituted sulphamides have been synthesised and their ionization equilibria in base (Schemes 1-3) have been studied.Many of the sulphamides are new materials.The pKa values obtained for each series have been correlated in Hammett and Taft plots.The Hammett ? values obtained for the ionization of the proximate hydrogen are ca. 2.3.The Taft ?* value obtained for ionization of the 'remoter' hydrogen is 1.68.The six-membered cyclic sulphamides are more acidic than their acyclic analogues by ca. 2.5 pKa units and the five-membered cyclic sulphamides are ca. 4 pKa units more acidic than model open-chain counterparts.Sulphur d-orbital involvement and ring-strain are suggested as possible sources of this 'acid-strengthening' effect.
