56100-69-7Relevant academic research and scientific papers
Design, synthesis and in vitro evaluation of novel SARS-CoV-2 3CLpro covalent inhibitors
Stille, Julia K.,Tjutrins, Jevgenijs,Wang, Guanyu,Venegas, Felipe A.,Hennecker, Christopher,Rueda, Andrés M.,Sharon, Itai,Blaine, Nicole,Miron, Caitlin E.,Pinus, Sharon,Labarre, Anne,Plescia, Jessica,Burai Patrascu, Mihai,Zhang, Xiaocong,Wahba, Alexander S.,Vlaho, Danielle,Huot, Mitchell J.,Schmeing, T. Martin,Mittermaier, Anthony K.,Moitessier, Nicolas
, (2022/01/08)
Severe diseases such as the ongoing COVID-19 pandemic, as well as the previous SARS and MERS outbreaks, are the result of coronavirus infections and have demonstrated the urgent need for antiviral drugs to combat these deadly viruses. Due to its essential role in viral replication and function, 3CLpro (main coronaviruses cysteine-protease) has been identified as a promising target for the development of antiviral drugs. Previously reported SARS-CoV 3CLpro non-covalent inhibitors were used as a starting point for the development of covalent inhibitors of SARS-CoV-2 3CLpro. We report herein our efforts in the design and synthesis of submicromolar covalent inhibitors when the enzymatic activity of the viral protease was used as a screening platform.
Leuckart-Wallach Route Toward Isocyanides and Some Applications
Neochoritis, Constantinos G.,Zarganes-Tzitzikas, Tryfon,Stotani, Silvia,D?mling, Adrian,Herdtweck, Eberhardt,Khoury, Kareem,D?mling, Alexander
supporting information, p. 493 - 499 (2015/09/22)
Isocyanide-based multicomponent reactions (IMCR) are among the most important chemical reactions to efficiently generate molecular diversity and have found widespread use in industry and academia. Generally, isocyanides are synthesized in 1-2 steps starting from primary amines. Here, we provide experimental detail on an alternative approach toward formamides and, thus, isocyanides via the Leuckart-Wallach reaction in an improved variation. The resulting >50 synthesized and characterized formamides are useful starting materials for IMCR, as well as other chemistries. The advantage of using the Leuckart-Wallach pathway to formamides and isocyanides is the lower price, on average, of the starting materials, as well as their differential and complementary structural diversity, as compared to the primary amine pathway.
A simple method for preparation of ZnO nanoparticles as a highly efficient nanocatalyst for N-formylation of primary and secondary amines under solvent-free condition
Alinezhad, Heshmatollah,Salehian, Fatemeh
, p. 532 - 538 (2013/07/19)
A convenient reaction between alky, aryl, and heteroalkyl amines and formic acid as a formylating agent in the presence of catalytic amount of mechanochemically synthesized zinc oxide nanoparticles under solvent-free condition for the synthesis of corresponding N-formyl derivatives is described. Copyright Taylor and Francis Group, LLC.
Identification and characterization of m4 selective muscarinic antagonists
Augelli-Szafran, Corinne E.,Jaen, Juan C.,Moreland, David W.,Nelson, Carrie B.,Penvose-Yi, Jan R.,Schwarz, Roy D.
, p. 1991 - 1996 (2007/10/03)
Our interest in the area of m4 muscarinic antagonists has led us to study a series of benzoxazine isoquinolines. One of the most potent and selective compounds of this series is example 1 with an IC50 value of 90.7nM at m4 receptors, and 72-fold (m1), 38-fold (m2), 10-fold (m3), and 82- fold (m5) more selective compared to the other receptors. The synthesis and receptor binding affinity of analogs of 1 are reported.
