939792-89-9Relevant articles and documents
Virtual Screening Approach to Identifying a Novel and Tractable Series of Pseudomonas aeruginosa Elastase Inhibitors
Leiris, Simon,Davies, David T.,Sprynski, Nicolas,Castandet, Jér?me,Beyria, Lilha,Bodnarchuk, Michael S.,Sutton, Jonathan M.,Mullins, Toby M. G.,Jones, Mark W.,Forrest, Andrew K.,Pallin, T. David,Karunakar, Paduri,Martha, Sathish Kumar,Parusharamulu, Battu,Ramula, Ramesh,Kotha, Venkatesh,Pottabathini, Narender,Pothukanuri, Srinivasu,Lemonnier, Marc,Everett, Martin
supporting information, p. 217 - 227 (2021/02/01)
Novel therapies are required to treat chronic bacterial infections in cystic fibrosis (CF) sufferers. The most common pathogen responsible for these infections is Pseudomonas aeruginosa, which persists within the lungs of CF sufferers despite intensive antibiotic treatment. P. aeruginosa elastase (also known as LasB or pseudolysin) is a key virulence determinant that contributes to the pathogenesis and persistence of P. aeruginosa infections in CF patients. The crucial role of LasB in pseudomonal virulence makes it a good target for the development of an adjuvant drug for CF treatment. Herein we discuss the discovery of a new series of LasB inhibitors by virtual screening and computer assisted drug design (CADD) and their optimization leading to compounds 29 and 39 (Ki = 0.16 μM and 0.12 μM, respectively).
CATALYST COMPOUNDS
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Paragraph 0314; 0321, (2015/03/28)
The present invention relates to an iridium-based catalyst compound for hydrogenating reducible moieties, especially imines and iminiums, the catalyst compounds being defined by the formulas: where ring B is either itself polycyclic, or ring B together with R is polycyclic. The catalysts of the invention are particularly effective in reductive amination procedures 10 which involve the in situ generation of the imine or iminium under reductive hydrogenative conditions.
CATALYST COMPOUNDS
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Paragraph 00163; 00170, (2013/11/05)
The present invention relates to an iridium-based catalyst compound for hydrogenating reducible moieties, especially imines and iminiums, the catalyst compounds being defined by the formulas: where ring B is either itself polycyclic, or ring B together with R is polycyclic. The catalysts of the invention are particularly effective in reductive amination procedures 10 which involve the in situ generation of the imine or iminium under reductive hydrogenative conditions.