X-ray crystallography-promoted drug design of carbonic anhydrase inhibitors
1-N-Alkylated-6-sulfamoyl saccharin derivatives were prepared and assayed as carbonic anhydrase inhibitors (CAIs). During X-ray crystallographic experiments an unexpected hydrolysis of the isothiazole ring was evidenced which allowed us to prepare highly
Glyoxalase 1 and 2 enzyme inhibitory activity of 6-sulfamoylsaccharin and sulfocoumarin derivates
The glyoxalase enzymes represent a cellular defence system against the accumulation of cytotoxic α-oxoaldehydes leading to apoptosis. The potential of glyoxalase inhibitors to act as novel anti-cancer agents for drugresistant tumours that over-express gly
Makrecka, Marina,Zalubovskis, Raivis,Vavers, Edijs,Ivanova, Jekaterina,Grandane, Aiga,Dambrova, Maija
p. 410 - 414
(2013/07/26)
Synthesis of 6-sulfamoylsaccharin and study of its reactivity in alkylation reactions
An improved method for the preparation of 6-sulfamoylsaccharin (3-oxo-2,3-dihydro-1,2-benzothiazole-6-sulfonamide 1,1-dioxide) has been developed and studies of its possible direct alkylation have been carried out. It was shown that alkylation occursregio
Ivanova,Simin, E. Yu.,Vozny,Trapencieris,?alubovskis
p. 1561 - 1564
(2018/01/27)
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