77278-77-4Relevant articles and documents
Sulfonamides incorporating piperazine bioisosteres as potent human carbonic anhydrase I, II, IV and IX inhibitors
Chiaramonte, Niccolò,Bua, Silvia,Angeli, Andrea,Ferraroni,Picchioni, Ilaria,Bartolucci, Gianluca,Braconi,Dei, Silvia,Teodori, Elisabetta,Supuran, Claudiu T.,Romanelli, Maria Novella
, (2019/08/01)
Starting from the molecular simplification of (R) 4-(3,4-dibenzylpiperazine-1-carbonyl)benzenesulfonamide 9a, a compound endowed with selectivity for human Carbonic Anhydrase (hCA) IV, a series of piperazines and 4-aminopiperidines carrying a 4-sulfamoylb
Novel bicyclic nitroimidazole carbamate compounds, process for preparation thereof and pharmaceutical composition for preventing or treating tuberculosis containing the same as an active ingredient
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, (2021/06/01)
A bicyclic nitroimidazole carbamate compound represented by chemical formula 1, an optical isomer thereof or a pharmaceutically acceptable salt thereof, a method for preparing the same, and a pharmaceutical composition for preventing or treating tuberculosis disease containing the same as an active ingredient. Chemical Formula 1. In Chemical Formula 1, R. 1 And R2 Are as defined in the description of the invention. The bicyclic nitroimidazole carbamate compounds of the present invention exhibit excellent inhibitory effects on vitality and non-active tuberculosis. The compounds can be useful in the treatment of tuberculosis.
Discovery of novel protease activated receptors 1 antagonists with potent antithrombotic activity in vivo
Perez, Michel,Lamothe, Marie,Maraval, Catherine,Mirabel, Etienne,Loubat, Chantal,Planty, Bruno,Horn, Clemens,Michaux, Julien,Marrot, Sebastien,Letienne, Robert,Pignier, Christophe,Bocquet, Arnaud,Nadal-Wollbold, Florence,Cussac, Didier,De Vries, Luc,Le Grand, Bruno
experimental part, p. 5826 - 5836 (2010/03/24)
Protease activated receptors (PARs) or thrombin receptors constitute a class of G-protein-coupled receptors (GPCRs) implicated in the activation of many physiological mechanisms. Thus, thrombin activates many cell types such as vascular smooth muscle cells, leukocytes, endothelial cells, and platelets via activation of these receptors. In humans, thrombin-induced platelet aggregation is mediated by one subtype of these receptors, termed PAR1. This article describes the discovery of new antagonists of these receptors and more specifically two compounds: 2-[5-oxo-5-(4-pyridin-2-ylpiperazin-1-yl)penta-1,3- dienyl]benzonitrile 36 (F 16618) and 3-(2-chlorophenyl)-1-[4-(4-fluorobenzyl) piperazin-1-yl]propenone 39 (F 16357), obtained after optimization. Both compounds are able to inhibit SFLLR-induced human platelet aggregation and display antithrombotic activity in an arteriovenous shunt model in the rat after iv or oral administration. Furthermore, these compounds are devoid of bleeding side effects often observed with other types of antiplatelet drugs, which constitutes a promising advantage for this new class of antithrombotic agents. 2009 American Chemical Society.