38191-33-2Relevant articles and documents
Direct Hydrogenation of Nitroaromatics at Room Temperature Catalyzed by Magnetically Recoverable Cu@Fe2O3 Nanoparticles
Borah, Biraj Jyoti,Bharali, Pankaj
, (2020/05/18)
Metal embedded in metal oxide nanoparticles are active as catalyst in plethora of industrially important reactions. Herein, embedded Cu@Fe2O3 nanoparticles was synthesized via a one step hydrothermal strategy which selectively catalyzes the hydrogenation of diverse nitroaromatics in H2O at room temperature. The remarkable catalytic performance is due to the successful hybridization of metallic Cu and Fe2O3 which in turn allows easy electroflipping between various oxidation states of Cu and Fe. Azo- and azoxy-compounds are not formed during the catalyzed process. This evidently establish that the hydrogenation of nitroaromatics proceeds via direct route with >99percent selectivity to the corresponding anilines.
Semi-quantitative models for identifying potent and selective transthyretin amyloidogenesis inhibitors
Connelly, Stephen,Mortenson, David E.,Choi, Sungwook,Wilson, Ian A.,Powers, Evan T.,Kelly, Jeffery W.,Johnson, Steven M.
supporting information, p. 3441 - 3449 (2017/07/07)
Rate-limiting dissociation of the tetrameric protein transthyretin (TTR), followed by monomer misfolding and misassembly, appears to cause degenerative diseases in humans known as the transthyretin amyloidoses, based on human genetic, biochemical and pharmacologic evidence. Small molecules that bind to the generally unoccupied thyroxine binding pockets in the native TTR tetramer kinetically stabilize the tetramer, slowing subunit dissociation proportional to the extent that the molecules stabilize the native state over the dissociative transition state—thereby inhibiting amyloidogenesis. Herein, we use previously reported structure-activity relationship data to develop two semi-quantitative algorithms for identifying the structures of potent and selective transthyretin kinetic stabilizers/amyloidogenesis inhibitors. The viability of these prediction algorithms, in particular the more robust in silico docking model, is perhaps best validated by the clinical success of tafamidis, the first-in-class drug approved in Europe, Japan, South America, and elsewhere for treating transthyretin aggregation-associated familial amyloid polyneuropathy. Tafamidis is also being evaluated in a fully-enrolled placebo-controlled clinical trial for its efficacy against TTR cardiomyopathy. These prediction algorithms will be useful for identifying second generation TTR kinetic stabilizers, should these be needed to ameliorate the central nervous system or ophthalmologic pathology caused by TTR aggregation in organs not accessed by oral tafamidis administration.
2-Aminobenzoxazole ligands of the hepatitis C virus internal ribosome entry site
Rynearson, Kevin D.,Charrette, Brian,Gabriel, Christopher,Moreno, Jesus,Boerneke, Mark A.,Dibrov, Sergey M.,Hermann, Thomas
supporting information, p. 3521 - 3525 (2014/07/22)
2-Aminobenzoxazoles have been synthesized as ligands for the hepatitis C virus (HCV) internal ribosome entry site (IRES) RNA. The compounds were designed to explore the less basic benzoxazole system as a replacement for the core scaffold in previously discovered benzimidazole viral translation inhibitors. Structure-activity relationships in the target binding of substituted benzoxazole ligands were investigated.