18942-49-9Relevant articles and documents
Enantiomeric discrimination of α-hydroxy acids and N-Ts-α-amino acids by1H NMR spectroscopy
Gao, Guangpeng,Lv, Caixia,Li, Qiuju,Ai, Lin,Zhang, Jiaxin
, p. 6742 - 6746 (2015)
A new kind of chiral compounds with multiple amino, amido and phenolic hydroxy groups has been synthesized from D-phenylalanine and D-phenylglycine, respectively. The enantiomeric discriminations of α-hydroxy acids and N-Ts-α-amino acids have been finished in the presence of the above chiral compounds as chiral solvating agents by1H NMR spectroscopy. The results show that the chiral compounds are highly effective and practical chiral solvating agents towards α-hydroxy acids and N-Ts-α-amino acids.
Novel irreversible covalent BTK inhibitors discovered using DNA-encoded chemistry
Guilinger, John P.,Archna, Archna,Augustin, Martin,Bergmann, Andreas,Centrella, Paolo A.,Clark, Matthew A.,Cuozzo, John W.,D?ther, Maike,Guié, Marie-Aude,Habeshian, Sevan,Kiefersauer, Reiner,Krapp, Stephan,Lammens, Alfred,Lercher, Lukas,Liu, Julie,Liu, Yanbin,Maskos, Klaus,Mrosek, Michael,Pflügler, Klaus,Siegert, Markus,Thomson, Heather A.,Tian, Xia,Zhang, Ying,Konz Makino, Debora L.,Keefe, Anthony D.
supporting information, (2021/06/15)
Libraries of DNA-Encoded small molecules created using combinatorial chemistry and synthetic oligonucleotides are being applied to drug discovery projects across the pharmaceutical industry. The majority of reported projects describe the discovery of reve
Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts
Le Manach, Claire,Dam, Jean,Woodland, John G.,Kaur, Gurminder,Khonde, Lutete P.,Brunschwig, Christel,Njoroge, Mathew,Wicht, Kathryn J.,Horatscheck, André,Paquet, Tanya,Boyle, Grant A.,Gibhard, Liezl,Taylor, Dale,Lawrence, Nina,Yeo, Tomas,Mok, Sachel,Eastman, Richard T.,Dorjsuren, Dorjbal,Talley, Daniel C.,Guo, Hui,Simeonov, Anton,Reader, Janette,Van Der Watt, Mari?tte,Erlank, Erica,Venter, Nelius,Zawada, Jacek W.,Aswat, Ayesha,Nardini, Luisa,Coetzer, Theresa L.,Lauterbach, Sonja B.,Bezuidenhout, Belinda C.,Theron, Anjo,Mancama, Dalu,Koekemoer, Lizette L.,Birkholtz, Lyn-Marie,Wittlin, Sergio,Delves, Michael,Ottilie, Sabine,Winzeler, Elizabeth A.,Smith, Dennis,Fidock, David A.,Street, Leslie J.,Basarab, Gregory S.,Duffy, James,Chibale, Kelly
, p. 2291 - 2309 (2021/03/01)
A novel diazaspiro[3.4]octane series was identified from a Plasmodium falciparum whole-cell high-throughput screening campaign. Hits displayed activity against multiple stages of the parasite lifecycle, which together with a novel sp3-rich scaffold provided an attractive starting point for a hit-to-lead medicinal chemistry optimization and biological profiling program. Structure-activity-relationship studies led to the identification of compounds that showed low nanomolar asexual blood-stage activity (50 nM) together with strong gametocyte sterilizing properties that translated to transmission-blocking activity in the standard membrane feeding assay. Mechanistic studies through resistance selection with one of the analogues followed by whole-genome sequencing implicated the P. falciparum cyclic amine resistance locus in the mode of resistance.
