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2 results on '"Adam Csakai"'

1. Tetrasubstituted imidazoles as incognito Toll-like receptor 8 a(nta)gonists

Author

Yi Yang, Adam Csakai, Shuangshuang Jiang, Christina Smith, Hiromi Tanji, Jian Huang, Torey Jones, Kentaro Sakaniwa, Lindsey Broadwell, Chengrui Shi, Subada Soti, Umeharu Ohto, Yaohui Fang, Shu Shen, Fei Deng, Toshiyuki Shimizu, and Hang Yin

Subjects
Science
Abstract

Toll-like receptor 8 (TLR8) plays essential roles in the innate immune response to viral single-stranded RNA (ssRNA), so small molecule modulators of TLR8 are of interest, however adverse effects limit their use. Here, the authors report a tetrasubstituted imidazole CU-CPD107 with dichotomous behaviour, which inhibits R848-induced TLR8 signaling, but shows synergistic activity in the presence of ssRNA, making it a potential antiviral agent.

Published
2021
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2. Multifunctional Building Blocks Compatible with Photoredox-Mediated Alkylation for DNA-Encoded Library Synthesis

Author

Weizhe Dong, Katelyn Billings, Adam Csakai, Xuange Zhang, Gary A. Molander, Jaehoon Sim, and Shorouk O. Badir

Subjects
Alkylation, 010402 general chemistry, 01 natural sciences, Biochemistry, Article, chemistry.chemical_compound, Physical and Theoretical Chemistry, Amines, Protecting group, Alkyl, chemistry.chemical_classification, Molecular Structure, 010405 organic chemistry, Extramural, Ligand, Organic Chemistry, Oxidation reduction, Stereoisomerism, Branching points, DNA, Photochemical Processes, Combinatorial chemistry, 0104 chemical sciences, Hydrocarbons, Brominated, chemistry, Oxidation-Reduction
Abstract

DNA-Encoded Library (DEL) technology has emerged as a novel interrogation modality for ligand discovery in the pharmaceutical industry. Given the increasing demand for a higher proportion of C(sp(3))-hybridized centers in DEL platforms, a photoredox-mediated cross-coupling and defluorinative alkylation process is introduced using commercially available alkyl bromides and structurally diverse α-silylamines. Notably, no protecting group strategies for amines are necessary for the incorporation of a variety of amino acid-based organosilanes, providing crucial branching points for further derivatization.

Published
2020

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