1‐Arylsulfonyl‐5‐(N‐hydroxyacrylamide)indolines Histone Deacetylase Inhibitors Are Potent Cytokine Release Suppressors

A series of 1‐arylsulfonyl‐5‐(N‐hydroxyacrylamide)indolines ( 7 – 15 ) has been developed; the compounds exhibited potent histone deacetylase (HDAC) inhibitory activities. Notably, almost all of this series exhibited better HDAC‐inhibitory and antiproliferative activities than 3‐(1‐benzenesulfonyl‐1H‐indol‐5‐yl)‐N‐hydroxyacrylamide ( 6 ), as reported in a previous study. Among these compounds, 3‐[1‐(4‐methoxybenzenesulfonyl)‐2,3‐dihydro‐1H‐indol‐5‐yl]‐N‐hydroxyacrylamide ( 9 ) showed a two‐ to tenfold increase in activity compared to SAHA ( 1 ) in the suppression of lipopolysaccharide‐induced cytokine production. Compound 9 also caused a marked reduction in carrageenan‐induced acute inflammation in a rat model. Taken together, these data indicated that 1‐arylsulfonyl‐5‐(N‐hydroxyacrylamide)indolines HDAC inhibitors exhibit potent anti‐inflammatory activity.     

Determination of Critical Aggregation Concentration in the Poly-(vinylpyrrolidone)–Sodium Dodecyl Sulfate System by Capillary Electrophoresis

We introduce an alternative separation method, i.e., capillary electrophoresis to examine the polymer/surfactant interaction. The migration behavior of the poly-(vinylpyrrolidone)–sodium dodecyl sulfate (PVP–SDS) model system was screened under a high electrical field for seven different PVP initial concentrations. From the electrophoretic mobilities of formed polymer–surfactant species, the critical aggregation concentration (CAC) of SDS for PVP was determined. The CAC value in the present study was very well matched with the CAC values of this system reported by alternative methods. A strong interaction between polymer and SDS under CAC concentration was observed and the independence of CAC on polymer concentration was experimentally demonstrated.     

Synthesis and decomposition performance of a polymeric foaming agent containing a sulfonyl hydrazide moiety

A new monomer, methacryloyloxybis(benzenesulfonyl hydrazide) (MAOBSH) containing a foamable sulfonyl hydrazide functional group after decomposition by heating, was synthesized from 4,4′‐oxybis(benzenesulfonyl hydrazide) (OBSH) with methacryloyl chloride, and used to obtain poly(MAOBSH) as a polymeric foaming agent (PFA) in dry tetrahydrofuran at 70 °C using azobisisobutyronitrile as an initiator. The structures of the synthesized MAOBSH and poly(MAOBSH) were identified using Fourier transform infrared and ¹ H NMR spectroscopies. The decomposition temperature of poly(MAOBSH) was determined to be 245 °C and this temperature was decreased to around 160 °C by adding an activator such as surface‐treated urea to the polymer. The exothermic temperature and heat determined by the decomposition of the polymer were 256 °C and 287 J g^?1. The amount of gas evolution for poly(MAOBSH) measured at the decomposition temperature was 74 mL g^?1. Furthermore, polymers incorporating the PFA showed better skin and finer cell structure as well as better mechanical properties such as elongation and compression set than polymers with added OBSH due to the better compatibility of the developed PFA with polymers. © 2012 Society of Chemical Industry