Results 161 to 170 of about 24,581 (324)

Development of New Benzo[b]Thiophene‐2‐Carboxamide Derivatives as Advanced Glycation End‐Products Receptor (RAGE) Antagonists

ChemMedChem, EarlyView.
A streamlined Ullmann‐Goldberg strategy enabled the synthesis of benzo[b]thiophene‐2‐carboxamides, promising ligands of the pro‐inflammatory RAGE receptor involved in inflammaging and age‐related diseases. LC‐MS, NMR, X‐ray and DFT studies elucidated the copper‐catalyzed mechanism. The lead compound, 3t’, shows inhibitory activity on the sRAGE/AGE2‐BSA
Lisa Bonin, Matthieu Hedouin, Christophe Furman, Ophélie Not, Steve Lancel, Mona Bensalah, Gael Coadou, Eric Boulanger, Sergiu Shova, Hassan Oulyadi, Alina Ghinet   +10 more
wiley   +1 more source

Allosteric Inhibitors of SARS‐CoV‐2 RNA‐Dependent RNA Polymerase Based on N,N′‐Diphenylurea

ChemMedChem, EarlyView.
Inhibitors of SARS‐CoV‐2 RdRp activity based on N,N′‐diphenylurea scaffold have been identified. Several compounds exhibit residual activity (RA) below 50% in an enzymatic assay (at 10 µM concentration) and improved aqueous solubility compared to the previously reported series of inhibitors.
Artem Chayka, Matěj Danda, Alžběta Dostálková, Vojtěch Spiwok, Lamija Zijadic, Anna Klimešová, Marina Kapisheva, Michala Zgarbová, Jan Weber, Tomáš Ruml, Michaela Rumlová, Zlatko Janeba   +11 more
wiley   +1 more source

Isomerization of N-acyl-1,2,5,6-tetrahydropyridines to N-acyl-enamines by palladium on carbon [PDF]

, 1987
Kärtner, Annerose, Wanner, Klaus Th.
core   +1 more source

Exploration and Characterization of the Antimalarial Activity of Pyrimidine‐2,4‐Diamines for which Resistance is Mediated by the ABCI3 Transporter

ChemMedChem, EarlyView.
Investigation of the structure‐activity relationship on W482 (1) with a pyrimidine‐2,4‐diamine scaffold culminated in analog 51 with enhanced anti‐plasmodial activity. Forward genetics and phenotypic examination revealed the ABCI3 transporter protein as a putative resistance mechanism.
Mahta Mansouri, Madeline G. Dans, Zijun Low, Katie Loi, Kate E. Jarman, Jocelyn S. Penington, Deyun Qiu, Adele M. Lehane, Benigno Crespo, Franciso‐Javier Gamo, Delphine Baud, Stephen Brand, Paul F. Jackson, Alan F. Cowman, Brad E. Sleebs   +14 more
wiley   +1 more source

Regio- and Stereocontrolled-Synthesis of a Heterocycle Fragment Collection Using Palladium Catalyzed C-H Arylation. [PDF]

Chemistry
Piticari AS, Antermite D, Linkhorn HJ, Larionova NA, Webster MP, Bull JA.   +5 more
europepmc   +1 more source

Efficient Synthesis of Cyclopropane-Fused Heterocycles with Bromoethylsulfonium Salt [PDF]

, 2013
Aggarwal, Artamonov, Basavaiah, Boger, Bornholdt, Catalan-Munoz, Chaplinski, de Carne-Carnavalet, Donohoe, Eckert, Feng, Fritz, Fritz, Fritz, Galeazzi, Gensini, Gomi, Gosselck, Gosselck, Greene, Hanessian, Hansch, Huang, Iwabuchi, Jeffery, Kamimura, Kasai, Kim, Kim, Kokotos, Krieter, Krow, Kulinkovich, Lin, Maeda, Mao, McGarrigle, McGarrigle, Meldrum, Miller, Namba, Nelson, Njoroge, Norris, Nunez, Ohno, Renslo, Sabbatini, Sasaki, Sattigeri, Schoepp, Shi, Takahashi, Tverezovsky, Unthank, Unthank, Van Zijl, Wiberg, Wirth, Xie, Xie, Xu, Yamanaka, Yar, Yar, Yar, Zhang   +66 more
core   +3 more sources

A Facile Protocol for C(sp2)–C(sp3) Bond Formation Reactions Toward Functionalized E3 Ligase Ligands

ChemMedChem, EarlyView.
A robust C(sp2)–C(sp3) decarboxylative coupling strategy enables access to new CRBN ligands and degraders with improved physicochemical properties. This synthetic approach is expanding the chemical space beyond C(sp2)–N linkages, fine‐tuning proteolysis‐targeting chimera activities and unlocking previously inaccessible degrader chemotypes.
Anita Maksutova, Thomas M. Geiger, Lorenzo Cianni, Dominika E. Pieńkowska, Jan Gerhartz, Lina Read, Aleša Bricelj, Alexander Herrmann, Maurice Leon Nelles, Yuen Lam Dora Ng, Marcus D. Hartmann, Jan Krönke, Izidor Sosič, Radosław P. Nowak, Michael Gütschow, Christian Steinebach   +15 more
wiley   +1 more source

Cooperative Brønsted Acid and Photo-Promoted Stereoselective Synthesis of Substituted Piperidones. [PDF]

Angew Chem Int Ed Engl
Peng Q, Mukherjee P, Suresh A, Hwang M, Gutierrez O, Scheidt KA.   +5 more
europepmc   +1 more source

Cycloaddition reactions for the synthesis of piperidine and indolizidine alkaloids [PDF]

, 1997
Andrew B. Holmes, Bernadette Bourdin, Ian Collins, E. C. DAVISON, Andrew J. Rudge, Thomas Stork, Jacqueline A. Warner   +6 more
openalex   +1 more source

Customizing Native Chemical Ligation: A Case Study on Histone Variant H2A.B from Toolbox to Target

Chemistry–Methods, EarlyView.
The core histone protein variant H2A.B, chosen as the target protein, is involved in many transcriptional processes regulated by its post‐translational modifications. Herein, the native chemical toolbox is harnessed to demonstrate the successful synthesis and semi‐synthesis of site‐specifically modified H2A.B variants via different strategies.
Tobias Gökler, Medine Soydan, Lydia Jane Barber, Garence Ferraton, Anne Claire Conibear   +4 more
wiley   +1 more source