65952-22-9Relevant academic research and scientific papers
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)
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.
Design, synthesis, and anticonvulsant activity of some sulfamides
Gavernet,Barrios,Cravero, M. Sella,Bruno-Blanch
, p. 5604 - 5614 (2008/03/14)
As part of our search for potential anticonvulsant agents, a set of compounds were designed, synthesized, and evaluated against MES and PTZ tests. Bioisosteric functional group information was used to design a new functionality, sulfamides, that complies with the requirements of the pharmacophore previously defined. Some of the molecules showed a promising anticonvulsant profile as selective anti-MES drugs, being active at low concentrations (30 mg/kg). The biological data were confirmed in Phase II of the Anticonvulsant Drug Development Program of the National Institute of Health.
Synthesis and antiprotozoal properties of 1,2,6-thiadiazine 1,1-dioxide derivatives
Herrero,Ochoa,Atienza,Escario,Gomez-Barrio,Martinez Fernandez
, p. 509 - 514 (2007/10/02)
The synthesis and spectroscopical data of 1,2,6-thiadiazine 1,1-dioxides, designed as antiprotozoal agents, are reported. The in vitro trichomonacidal and trypanocidal activities of new compounds and their precursors were evaluated against Trichomonas vag
Intra- and Intermolecular α-Sulfamidoalkylation Reactions
Lee, Chai-Ho,Kohn, Harold
, p. 6098 - 6104 (2007/10/02)
The utility of α-sulfamidoalkylation processes for the generation of sulfamides has been examined.Select aryl-substituted sulfamides were prepared and then treated with acid.Both intra- and intermolecular α-sulfamidoalkylation transformations were observed to proceed in moderate to good yields.The pathways for these reactions are discussed.The generality of these processes has been demonstrated using N,N'-di(aryl-substituted)sulfamides, and the utility of these reactions was examined for the preparation of cyclic sulfamides of novel structure.
