147000-78-0Relevant articles and documents
Synthesis and antitumor evaluation of novel sulfonylcycloureas derived from nitrogen mustard
Cheloufi,Belhani,Ouk,Zerrouki,Aouf,Berredjem
, p. 399 - 405 (2016/04/20)
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 (2am) with ethyl bis(2-chloroethyl)carbamate (1a). The relative cytotoxicity of these new derivatives in comparison to chlorambucil is reported.
SULFAMIDE LINKER, CONJUGATES THEREOF, AND METHODS OF PREPARATION
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Page/Page column 100, (2016/04/26)
The present invention relates to a compound comprising an alpha-end and an omega-end, the compound comprising on the alpha-end a reactive group Qlcapable of reacting with a functional group F1present on a biomolecule and on the omega-end a target molecule, the compound further comprising a group according to formula (1) or a salt thereof: Said compound may also be referred to as a linker-conjugate. The invention also relates to a process for the preparation of a bioconjugate, the process comprising the step of reacting a reactive group Q1of a linker-conjugate according to the invention with a functional group F1of a biomolecule. The invention further relates to a bioconjugate obtainable by the process according to the invention. In a preferred embodiment, the invention concerns a process for the preparation of a bioconjugate via a cycloaddition, such as a (4+2)-cycloaddition (e.g. a Diels-Alder reaction) or a (3+2)-cycloaddition (e.g. a 1,3-dipolar cycloaddition).
Simple, rapid, and clean condensation of sulfonamide and maleic anhydride derivatives: Synthesis of novel 1H- Pyrrole-2,5-diones under heterogeneous conditions
Bougheloum, Chafika,Guezane Lakoud, Samia,Belghiche, Robila,Messalhi, Abdelrani
supporting information, p. 1344 - 1350 (2016/09/28)
H6P2W18O62is used as an efficient catalyst for the synthesis of novel N-substituted sulfonyl maleimides (1H-Pyrrole-2,5-diones) via the condensation of sulfonamide and maleic anhydride derivatives. The Dawson heteropolyacid was used with a catalytic amount of 2?mmol% in acetonitrile at reflux. The reuse of H6P2W18O62as heterogeneous catalyst several times without decrease in their activity, short reaction times, easy isolation of desired products with good to excellent yields shows the advantages of this novel methodology.
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
Synthesis of new substituted N-sulfonyl pyrrolidine-2,5-dione using dawson-type heteropolyacid as catalyst
Bougheloum, Chafika,Belghiche, Robila,Messalhi, Abdelrani
supporting information, p. 269 - 276 (2015/04/27)
The synthesis of new series of pyrrolidine-2,5-diones having sulfonamide moieties is described. These compounds are synthesized in good yield in three steps (carbamoylation-sulfamoylation, deprotection and condensation) using a catalytic amount of H6P2W18O62 in acetonitrile under refluxing conditions.
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.
Hypervalent iodine reagent mediated diamination of [60]fullerene with sulfamides or phosphoryl diamides
Yang, Hai-Tao,Lu, Xin-Wei,Xing, Meng-Lei,Sun, Xiao-Qiang,Miao, Chun-Bao
supporting information, p. 5882 - 5885 (2015/02/19)
A hypervalent iodine-promoted intermolecular diamination reactions of C60 with sulfamides or phosphoryl diamides affords two classes of novel C60-fused cyclic sulfamide or phosphoryl diamide derivatives. The reaction between C60 and sulfamides can be effectively controlled to selectively synthesize diamination products or azafulleroids under PhIO/I2 or PhI(OAc)2/I2 conditions, respectively. Moreover, phosphoryl diamides were first used as an amine source in the diamination of alkenes.
Inhibition pattern of sulfamide-related compounds in binding to carbonic anhydrase isoforms I, II, VII, XII and XIV
Gavernet, Luciana,Gonzalez Funes, Jose L.,Palestro, Pablo H.,Bruno Blanch, Luis E.,Estiu, Guillermina L.,Maresca, Alfonso,Barrios, Ivana,Supuran, Claudiu T.
, p. 1410 - 1418 (2013/04/10)
A set of sulfamides and sulfamates were synthesized and tested against several isoforms of carbonic anhydrase: CA I, CA II, CA VII, CA XII and CA XIV. The biological assays showed a broad range of inhibitory activity, and interesting results were found for several compounds in terms of activity (Ki 1 μm) and selectivity: some aromatic sulfamides are active against CA I, CA II and/or CA VII; while they are less active in CA XII and CA XIV. On the other hand, bulky sulfamides are selective to CA VII. To understand the origin of the different inhibitory activity against each isozyme we used molecular modeling techniques such as docking and molecular dynamic simulations.
4-PYRIMIDINESULFAMIDE DERIVATIVE
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Page/Page column 4, (2012/06/16)
The invention relates to the compound of structural formula (I) and the salts thereof. Said compound is useful as endothelin receptor antagonist. The invention further relates to a process for preparing said compound.
Alternative synthetic strategies for new drug candidates. The thermolysis reaction of N-(benzyl)-N′-(tert-butoxycarbonyl)sulfamide to yield benzylsulfamide
Lick,Gavernet,Bruno-Blanch,Ponzi
scheme or table, p. 30 - 34 (2010/07/04)
The hydrolysis of one sulfamide derivative under conventional conditions and under thermolysis reaction has been investigated. Comparison between these techniques revealed advantages in the use of thermal decomposition reaction to obtain sulfamides, due to the easy elimination of gaseous by-products produced in the reaction.
