1755-45-9Relevant articles and documents
Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors
Albrecht, Brian K.,Audia, James E.,Balasubramanian, Srividya,Bellon, Steven F.,Brucelle, Francois,Cummings, Richard T.,Duplessis, Martin,Gehling, Victor S.,Good, Andrew C.,Harmange, Jean-Christophe,Iyer, Priyadarshini,Khanna, Avinash,Levell, Julian R.,McGrath, John P.,Sawant, Priyanka,Stuckey, Jacob,Trojer, Patrick,Vaswani, Rishi G.,Watson, Venita,C?té, Alexandre
, p. 1213 - 1220 (2020)
Leveraging the catalytic machinery of LSD1 (KDM1A), a series of covalent styrenylcyclopropane LSD1 inhibitors were identified. These inhibitors represent a new class of mechanism-based inhibitors that target and covalently label the FAD cofactor of LSD1.
Asymmetric Nazarov Cyclizations of Unactivated Dienones by Hydrogen-Bond-Donor/Lewis Acid Co–Catalyzed, Enantioselective Proton-Transfer
Metternich, Jan B.,Reiterer, Martin,Jacobsen, Eric N.
supporting information, p. 4092 - 4097 (2020/09/01)
We report an enantioselective Nazarov cyclization catalyzed by chiral hydrogen-bond-donors in concert with silyl Lewis acids. The developed transformation provides access to tri-substituted cyclopentenones in high levels of enantioselectivity (up to 95% e.e.) from a variety of simple unactivated dienones. Kinetic and mechanistic studies are consistent with a reversible 4π-electrocyclization C?C bond-forming step followed by rate- and enantio-determining proton-transfer as the mode of catalysis. (Figure presented.).
INHIBITORS OF METALLO-BETA-LACTAMASES
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Paragraph 00225; 00226, (2018/12/13)
The present invention relates to compounds of Formula (I) that function as inhibitors of bacterial metallo-beta-lactamases. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of a bacterial infection. (Formula (I))
