1126-09-6Relevant articles and documents
Synthesis and SAR studies of 1-substituted-n-(4-alkoxycarbonylpiperidin-1-yl)alkanes as potent antiarrhythmic agents
Tripathi, Ravish C.,Pandey, Suresh K.,Kar,Dikshit,Saxena, Anil K.
, p. 2693 - 2698 (1999)
Synthesis and SAR studies of the title compounds have resulted in the identification of structural and physicochemical parameter (Vw) contributing for antiarrhythmic activity. Among the two most promising compounds 3a and 3b, the 3a has shown antiarrhythmic activity comparable to quinidine.
A novel approach for the synthesis of hydrogel nanoparticles and a removal study of reactive dyes from industrial effluent
Mahida, Viran P.,Patel, Manish P.
, p. 21577 - 21589 (2016)
A novel amphoteric monomer, N,N-diallyl carboxypiperidinium bromide (DACPB), has been synthesized by the stepwise condensation of isonipecotic acid to an ester and then with allyl chloride and allyl bromide. The present research study highlights the UV-irradiation synthesis of poly(NIPAAm/DACPB/APTAC) superabsorbent nanohydrogels by free radical polymerization. Nanohydrogel (VUV-05) shows faster swelling and a greater swelling percentage (～43000%), which was responsible for the high adsorption of dyes, than that in our previous research study. The synthesized nanohydrogel (VUV-05) was applied for a removal study of Reactive Red 152 dye from industrial effluent. Also, a removal study for a mixture of three reactive dyes, namely Reactive Red 195, Reactive Blue 222 and Reactive Black 5, was carried out from a sole industrial effluent. The nanohydrogels with and without dye adsorption were characterized by FT-IR, TGA, SEM and zeta potential analysis. The effect of parameters such as the initial dye concentration, treatment time, pH, and adsorbent dose were investigated to determine the maximum adsorption. From the removal study it was observed that ～87% of RR-152 dye can be removed from industrial effluent. Also, the nanohydrogel was able to remove the mixture of reactive dyes, and its removal efficiency was 53.14%, 51.90% and 51.06% for RR-195, RB-222 and RB-5 from a lone industrial effluent (30%), respectively. After the removal study, it was concluded that the pseudo-second order and Langmuir models may well describe the Reactive Red 152 dye adsorption process.
Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor
Granchi, Carlotta,Lapillo, Margherita,Glasmacher, Sandra,Bononi, Giulia,Licari, Cristina,Poli, Giulio,El Boustani, Maguie,Caligiuri, Isabella,Rizzolio, Flavio,Gertsch, Jürg,Macchia, Marco,Minutolo, Filippo,Tuccinardi, Tiziano,Chicca, Andrea
, p. 1932 - 1958 (2019/02/26)
Monoacylglycerol lipase (MAGL) is the enzyme degrading the endocannabinoid 2-arachidonoylglycerol, and it is involved in several physiological and pathological processes. The therapeutic potential of MAGL is linked to several diseases, including cancer. The development of MAGL inhibitors has been greatly limited by the side effects associated with the prolonged MAGL inactivation. Importantly, it could be preferable to use reversible MAGL inhibitors in vivo, but nowadays only few reversible compounds have been developed. In the present study, structural optimization of a previously developed class of MAGL inhibitors led to the identification of compound 23, which proved to be a very potent reversible MAGL inhibitor (IC50 = 80 nM), selective for MAGL over the other main components of the endocannabinoid system, endowed of a promising antiproliferative activity in a series of cancer cell lines and able to block MAGL both in cell-based as well as in vivo assays.
Polysilane-Immobilized Rh-Pt Bimetallic Nanoparticles as Powerful Arene Hydrogenation Catalysts: Synthesis, Reactions under Batch and Flow Conditions and Reaction Mechanism
Miyamura, Hiroyuki,Suzuki, Aya,Yasukawa, Tomohiro,Kobayashi, Shu
supporting information, p. 11325 - 11334 (2018/09/06)
Hydrogenation of arenes is an important reaction not only for hydrogen storage and transport but also for the synthesis of functional molecules such as pharmaceuticals and biologically active compounds. Here, we describe the development of heterogeneous Rh-Pt bimetallic nanoparticle catalysts for the hydrogenation of arenes with inexpensive polysilane as support. The catalysts could be used in both batch and continuous-flow systems with high performance under mild conditions and showed wide substrate generality. In the continuous-flow system, the product could be obtained by simply passing the substrate and 1 atm H2 through a column packed with the catalyst. Remarkably, much higher catalytic performance was observed in the flow system than in the batch system, and extremely strong durability under continuous-flow conditions was demonstrated (>50 days continuous run; turnover number >3.4 × 105). Furthermore, details of the reaction mechanisms and the origin of different kinetics in batch and flow were studied, and the obtained knowledge was applied to develop completely selective arene hydrogenation of compounds containing two aromatic rings toward the synthesis of an active pharmaceutical ingredient.
