22245-96-1Relevant articles and documents
1,2,4-Triazole-3-Thione Analogues with a 2-Ethylbenzoic Acid at Position 4 as VIM-type Metallo-β-Lactamase Inhibitors
Benvenuti, Manuela,Bouajila, Ezeddine,Cerboni, Giulia,Chelini, Giulia,Corsica, Giuseppina,De Luca, Filomena,Docquier, Jean-Denis,Feller, Georges,Galleni, Moreno,Gavara, Laurent,Hernandez, Jean-Fran?ois,Legru, Alice,Licznar-Fajardo, Patricia,Mangani, Stefano,Mercuri, Paola Sandra,Pozzi, Cecilia,Sannio, Filomena,Sevaille, Laurent,Tanfoni, Silvia,Tassone, Giusy,Verdirosa, Federica,Vo Hoang, Yen
, (2022/02/16)
Metallo-β-lactamases (MBLs) are increasingly involved as a major mechanism of resistance to carbapenems in relevant opportunistic Gram-negative pathogens. Unfortunately, clinically efficient MBL inhibitors still represent an unmet medical need. We previou
Cyclic-fused ASK1 inhibitor and application thereof
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Paragraph 0212-0215, (2019/10/15)
The invention relates to a cyclic-fused ASK1 inhibitor and application thereof, and particularly to a compound shown in formula (I), a pharmacologically acceptable salt and ester thereof, and a stereisomer thereof. The invention further relates to a preparation method of the compound, a pharmaceutic preparation and a pharmaceutical composition containing the compound. The compound of the inventionis capable of effectively inhibiting phosphorylation of amino acid of ASK1, and inhibiting the activation of the ASK1, thereby can be used for treating and/or preventing ASK1-mediated diseases and related diseases.
Facile synthesis of 5-To 7-membered benzolactam compounds via strongly facilitated electrophilic aromtic substitution reaction
Kurouchi, Hiroaki,Otani, Yuko,Ohwada, Tomohiko
, p. 705 - 713 (2017/04/10)
We employed our system to activate aromatic ring-Tethered carbamate compounds with trifluoromethanesulfonic acid to obtain benzolactams with 5-To 7-membered rings, and examined the substrate scope and limitations of this activation method. In 5-membered ring formation, a halogen group on the aromatic ring did not greatly affect the reaction yield, but other electron-donating groups inhibited the cyclization reaction, and various side-reactions occurred. In 7-membered ring formation, eletron-donating groups on aromatic ring promoted the cyclization reaction, but cyclization of electron-deficient aromatic rings did not proceed well. The 6-membered ring formation reaction showed the greatest substrate generality.