186590-23-8Relevant articles and documents
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria
Lapointe, Guillaume,Skepper, Colin K.,Holder, Lauren M.,Armstrong, Duncan,Bellamacina, Cornelia,Blais, Johanne,Bussiere, Dirksen,Bian, Jianwei,Cepura, Cody,Chan, Helen,Dean, Charles R.,De Pascale, Gianfranco,Dhumale, Bhavesh,Fisher, L. Mark,Fulsunder, Mangesh,Kantariya, Bhavin,Kim, Julie,King, Sean,Kossy, Lauren,Kulkarni, Upendra,Lakshman, Jay,Leeds, Jennifer A.,Ling, Xiaolan,Lvov, Anatoli,Ma, Sylvia,Malekar, Swapnil,McKenney, David,Mergo, Wosenu,Metzger, Louis,Mhaske, Keshav,Moser, Heinz E.,Mostafavi, Mina,Namballa, Sunil,Noeske, Jonas,Osborne, Colin,Patel, Ashish,Patel, Darshit,Patel, Tushar,Piechon, Philippe,Polyakov, Valery,Prajapati, Krunal,Prosen, Katherine R.,Reck, Folkert,Richie, Daryl L.,Sanderson, Mark R.,Satasia, Shailesh,Savani, Bhautik,Selvarajah, Jogitha,Sethuraman, Vijay,Shu, Wei,Tashiro, Kyuto,Thompson, Katherine V.,Vaarla, Krishniah,Vala, Lakhan,Veselkov, Dennis A.,Vo, Jason,Vora, Bhavesh,Wagner, Trixie,Wedel, Laura,Williams, Sarah L.,Yendluri, Satya,Yue, Qin,Yifru, Aregahegn,Zhang, Yong,Rivkin, Alexey
supporting information, p. 6329 - 6357 (2021/06/01)
Herein, we describe the discovery and optimization of a novel series that inhibits bacterial DNA gyrase and topoisomerase IV via binding to, and stabilization of, DNA cleavage complexes. Optimization of this series led to the identification of compound 25
Stereoselective Access to 1-[2-Bromo(het)aryloxy]propan-2-amines Using Transaminases and Lipases; Development of a Chemoenzymatic Strategy Toward a Levofloxacin Precursor
Mourelle-Insua, ángela,López-Iglesias, María,Gotor, Vicente,Gotor-Fernández, Vicente
, p. 9765 - 9774 (2016/10/31)
Two independent enzymatic strategies have been developed toward the synthesis of enantioenriched 1-[2-bromo(het)aryloxy]propan-2-amines. With that purpose a series of racemic amines and prochiral ketones have been synthesized from commercially available 2-bromophenols or brominated pyridine derivatives bearing different pattern substitutions in the aromatic ring. Biotransamination experiments have been studied using ketones as starting materials, yielding both the (R)- and (S)-amine enantiomers with high selectivity (91-99% ee) depending on the transaminase source. In a complementary approach, the classical kinetic resolutions of the racemic amines have been investigated using Candida antarctica lipase type B as biocatalyst. Ethyl methoxyacetate was found as a suitable acyl donor leading to the corresponding (S)-amines (90-99% ee) and (R)-amides (88-99% ee) with high selectivity in most of the cases. A preparative biotransamination process has been developed for the synthesis of (2S)-1-(6-bromo-2,3-difluorophenoxy)propan-2-amine in 61% isolated yield after 24 h, a valuable precursor of the antimicrobial agent Levofloxacin.
RADIOLABELLED mGluR2 PET LIGANDS
-
Paragraph 0194, (2013/09/12)
The present invention relates to novel, selective, radiolabelled mGluR2 ligands which are useful for imaging and quantifying the metabotropic glutamate receptor mGluR2 in tissues, using positron-emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo and to precursors of said compounds.