98432-01-0Relevant articles and documents
Discovery of Novel Inhibitors of Uridine Diphosphate- N-Acetylenolpyruvylglucosamine Reductase (MurB) from Pseudomonas aeruginosa, an Opportunistic Infectious Agent Causing Death in Cystic Fibrosis Patients
Abell, Chris,Blundell, Tom L.,Brown, Karen P.,Coyne, Anthony G.,Di Pietro, Ornella,Floto, R. Andres,Hess, Jeannine,Holland, Matthew T. O.,Kim, So Yeon,Marchetti, Chiara,Mendes, Vitor,Acebrón-García-De-Eulate, Marta,Mayol-Llinàs, Joan
, p. 2149 - 2173 (2022/02/14)
Pseudomonas aeruginosa is of major concern for cystic fibrosis patients where this infection can be fatal. With the emergence of drug-resistant strains, there is an urgent need to develop novel antibiotics against P. aeruginosa. MurB is a promising target
Highly Diastereo- and Enantioselective Access to syn-α-Amido β-Hydroxy Esters via Ruthenium-Catalyzed Dynamic Kinetic Resolution-Asymmetric Hydrogenation
Lu, Bin,Wu, Xiaoyu,Li, Chengyang,Ding, Guangni,Li, Wanfang,Xie, Xiaomin,Zhang, Zhaoguo
, p. 3201 - 3213 (2019/03/11)
Dynamic kinetic resolution (DKR) of racemic aryl α-amino β-ketoesters via Ru-diphosphine-catalyzed asymmetric hydrogenation was realized at 70 °C under 50 atm of hydrogen, affording syn α-amido β-hydroxy esters in high yields (up to 96%) with high reactivity (TON up to 940) and diastereo- and enantioselectivities (up to 99:1 dr, 98% ee). These hydrogenation products provide valuable chiral synthons in many natural products and pharmaceuticals. Gram-scale DKR asymmetric hydrogenation (DKR-AH) was also performed with retained reactivity and stereoselectivity, revealing the synthetic utility of this method.
Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies
Lange, Jos H.M.,van der Neut, Martina A.W.,Wals, Henri C.,Kuil, Gijs D.,Borst, Alice J.M.,Mulder, Arie,den Hartog, Arnold P.,Zilaout, Hicham,Goutier, Wouter,van Stuivenberg, Herman H.,van Vliet, Bernard J.
supporting information; experimental part, p. 1084 - 1089 (2010/06/11)
The synthesis and structure-activity relationship studies of imidazoles are described. The target compounds 6-20 represent a novel chemotype of potent and CB2/CB1 selective cannabinoid CB2 receptor antagonists/inverse agonists with very high binding efficiencies in combination with favourable log P and calculated polar surface area values. Compound 12 exhibited the highest CB2 receptor affinity (Ki = 1.03 nM) in this series, as well as the highest CB2/CB1 subtype selectivity (>9708-fold).
