4254-32-4Relevant 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).
N-Atom Deletion in Nitrogen Heterocycles
Qin, Haitao,Cai, Wangshui,Wang, Shuang,Guo, Ting,Li, Guigen,Lu, Hongjian
, p. 20678 - 20683 (2021/08/25)
Excising the nitrogen in secondary amines, and coupling the two residual fragments is a skeletal editing strategy that can be used to construct molecules with new skeletons, but which has been largely unexplored. Here we report a versatile method of N-atom excision from N-heterocycles. The process uses readily available N-heterocycles as substrates, and proceeds by N-sulfonylazidonation followed by the rearrangement of sulfamoyl azide intermediates, providing various cyclic products. Examples are provided of deletion of nitrogen from natural products, synthesis of chiral O-heterocycles from commercially available chiral β-amino alcohols, formal inert C?H functionalization through a sequence of N-directed C?H functionalization and N-atom deletion reactions in which the N-atom can serve as a traceless directing group.
INDANE DERIVATIVES FOR USE IN THE TREATMENT OF BACTERIAL INFECTION
-
Paragraph 0093; 0104-0105, (2020/04/09)
The invention relates to a compound which is an indane according to Formula (I), or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, n and p are as defined herein