76875-21-3Relevant articles and documents
Targeting the FtsZ Allosteric Binding Site with a Novel Fluorescence Polarization Screen, Cytological and Structural Approaches for Antibacterial Discovery
Huecas, Sonia,Araújo-Bazán, Lidia,Ruiz, Federico M.,Ruiz-ávila, Laura B.,Martínez, R. Fernando,Escobar-Pe?a, Andrea,Artola, Marta,Vázquez-Villa, Henar,Martín-Fontecha, Mar,Fernández-Tornero, Carlos,López-Rodríguez, María L.,Andreu, José M.
supporting information, p. 5730 - 5745 (2021/06/01)
Bacterial resistance to antibiotics makes previously manageable infections again disabling and lethal, highlighting the need for new antibacterial strategies. In this regard, inhibition of the bacterial division process by targeting key protein FtsZ has been recognized as an attractive approach for discovering new antibiotics. Binding of small molecules to the cleft between the N-terminal guanosine triphosphate (GTP)-binding and the C-terminal subdomains allosterically impairs the FtsZ function, eventually inhibiting bacterial division. Nonetheless, the lack of appropriate chemical tools to develop a binding screen against this site has hampered the discovery of FtsZ antibacterial inhibitors. Herein, we describe the first competitive binding assay to identify FtsZ allosteric ligands interacting with the interdomain cleft, based on the use of specific high-affinity fluorescent probes. This novel assay, together with phenotypic profiling and X-ray crystallographic insights, enables the identification and characterization of FtsZ inhibitors of bacterial division aiming at the discovery of more effective antibacterials.
Four-tooth-ring metal palladium (II) complex phosphorescent material
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Paragraph 0067; 0068, (2018/03/24)
The invention discloses a four-tooth-ring metal palladium (II) complex phosphorescent material represented by a formula (I), wherein a pentabasic heteromatic group Ar is formula (shown in the description) and is selected from one of the following formulae: 2H-1,2,3-triazole, wherein X1 is equal to N, X2 is equal to N, and X3 is equal to CH); 1H-1,2,3-triazole, wherein X1 is equal to CH, X2 is equal to N, and X3 is equal to N; oxazole, wherein X1 is equal to O, X2 is equal to C, and X3 is equal to CH; thiazole, X1 is equal to S, X2 is equal to C, and X3 is equal to CH; or N-methylimidazole, wherein X1 is equal to N-Me, X2 is equal to C, and X3 is equal to CH). The four-tooth-ring metal palladium (II) complex phosphorescent material is strong in molecular rigidity, capable of effectively reducing energy consumed by molecular vibration, high in phosphorescent quantum efficiency and good in chemical stability and thermal stability and can be applied to luminescent layers of organic luminescent devices.
An efficient synthesis of 2-arylimidazoles by oxidation of 2-arylimidazolines using activated carbon-O2 system and its application to palladium-catalyzed Mizoroki-Heck reaction
Haneda, Satoshi,Okui, Ayaka,Ueba, Chigusa,Hayashi, Masahiko
, p. 2414 - 2417 (2007/10/03)
Oxidative conversion of 2-substituted imidazoline (dihydroimidazole) to the corresponding imidazole was achieved by an activated carbon-O2 system. Also, the 2-arylimidazolines and 2-arylimidazoles have been found to work as simple ligands in the palladium-catalyzed Mizoroki-Heck reaction.