Hydroxamic acid with benzenesulfonamide: An effective scaffold for the development of broad-spectrum metallo-β-lactamase inhibitors
Given that β-lactam antibiotic resistance mediated by metallo-β-lactamases (MβLs) seriously threatens human health, we designed and synthesized nineteen hydroxamic acids with benzenesulfonamide, which exhibited broad-spectrum inhibition against four teste
Some 4-(substituted phenylsulfonamido)benzoic acids have been synthesized by fly-ash:H3PO3 nano catalyst catalyzed condensation of substituted benzenesulfonyl chlorides and 4-aminobenzoic acid in ultrasound irradiation conditions. The yields of the sulfonamides are more than 90%. The synthesized 4-(substituted phenylsulfonamido) benzoic acid derivatives were characterized by their physical constants, analytical and spectroscopic data. Antimicrobial activities of all sulfonamides were measured by Bauer-Kirby disc diffusion method.
Solid-phase parallel synthesis and SAR of 4-amidofuran-3-one inhibitors of cathepsin S: Effect of sulfonamides P3 substituents on potency and selectivity
Highly potent and selective 4-amidofuran-3-one inhibitors of cathepsin S are described. The synthesis and structure-activity relationship of a series of inhibitors with a sulfonamide moiety in the P3 position is presented. Several members of the series show sub-nanomolar inhibition of the target enzyme as well as an excellent selectivity profile and good cellular potency. Molecular modeling of the most interesting inhibitors describes interactions in the extended S3 pocket and explains the observed selectivity towards cathepsin K.
The present invention relates to hydroxamic acid derivatives that are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the
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Page/Page column 15
(2010/11/29)
Kinetics of arylsulfonation of aminobenzoic acids with m-and p-nitrobenzenesulfonyl chlorides in the system water-2-propanol
The concentrations of the uncharged and anionic forms of m-and p-aminobenzoic acids participating in arylsulfonation of the acids with m-and p-nitrobenzenesulfonyl chlorides in the system water-2-propanol at 298 K at various water contents and pHs were estimated. The resulting data were used to estimate the rate constants for the reactions of the above forms with nitrobenzenesulfonyl chlorides, based on experimental kinetic data.
Kustova,Kuritsyn,Khripkova
p. 623 - 626
(2007/10/03)
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