22246-05-5Relevant 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
supporting information, (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
AMINE COMPOUND FOR INHIBITING SSAO / VAP-1 AND USE THEREOF
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Paragraph 0287; 0415-0417, (2020/12/13)
An amine compound serving as a semicarbazide-sensitive amine oxidase (SSAO) and/or vascular adhesion protein-1 (VAP-1) inhibitor, a pharmaceutical composition, and an application thereof in medicines that can be used for treating inflammation and/or inflammation related diseases, diabetes and/or a disease related diabetes, psychiatric disorder, ischemic disease, vascular disease, fibrosis, or tissue transplant rejection.
Synthesis and pharmacological evaluation of new 3,4-dihydroisoquinolin derivatives containing heterocycle as potential anticonvulsant agents
Zhang, Hong-Jian,Shen, Qing-Kun,Jin, Chun-Mei,Quan, Zhe-Shan
, (2016/12/16)
Two novel series of 3,4-dihydroisoquinolin with heterocycle derivatives (4a-t and 9a-e) were synthesized and evaluated for their anticonvulsant activity using maximal electroshock (MES) test and pentylenetetrazole (PTZ)-induced seizure test. All compounds were characterized by IR, 1H-NMR, 13C-NMR, and mass spectral data. Among them, 9-(exyloxy)-5,6-dihydro-[1,2,4]triazolo[3,4-a] isoquinolin-3(2H)-one (9a) showed significant anticonvulsant activity in MES tests with an ED50 value of 63.31 mg/kg and it showed wide margins of safety with protective index (PI > 7.9). It showed much higher anticonvulsant activity than that of valproate. It also demonstrated potent activity against PTZ-induced seizures. A docking study of compound 9a in the benzodiazepine (BZD)-binding site of γ-aminobutyric acidA (GABAA) receptor confirmed possible binding of compound 9a with the BZD receptors.