24260-30-8Relevant academic research and scientific papers
Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis
Boiteau, Jean-Guy,Ouvry, Gilles,Arlabosse, Jean-Marie,Astri, Stéphanie,Beillard, Audrey,Bhurruth-Alcor, Yushma,Bonnary, Laetitia,Bouix-Peter, Claire,Bouquet, Karine,Bourotte, Marilyne,Cardinaud, Isabelle,Comino, Catherine,Deprez, Beno?t,Duvert, Denis,Féret, Angélique,Hacini-Rachinel, Feriel,Harris, Craig S.,Luzy, Anne-Pascale,Mathieu, Arnaud,Millois, Corinne,Orsini, Nicolas,Pascau, Jonathan,Pinto, Artur,Piwnica, David,Polge, Ga?lle,Reitz, Arnaud,Reversé, Kevin,Rodeville, Nicolas,Rossio, Patricia,Spiesse, Delphine,Tabet, Samuel,Taquet, Nathalie,Tomas, Lo?c,Vial, Emmanuel,Hennequin, Laurent F.
supporting information, p. 945 - 956 (2018/02/20)
Targeting the TNFα pathway is a validated approach to the treatment of psoriasis. In this pathway, TACE stands out as a druggable target and has been the focus of in-house research programs. In this article, we present the discovery of clinical candidate
Studies on novel 2-imidazolidinones and tetrahydropyrimidin-2(1H)-ones as potential TACE inhibitors: Design, synthesis, molecular modeling, and preliminary biological evaluation
DasGupta, Shirshendu,Murumkar, Prashant R.,Giridhar, Rajani,Yadav, Mange Ram
experimental part, p. 3604 - 3617 (2009/09/30)
Compounds belonging to the class of 2-imidazolidinones and tetrahydropyrimidin-2(1H)-ones were synthesized and evaluated for their TACE inhibitory activity. Most of the compounds showed very good TACE inhibitory activity. Docking study clearly indicates importance of the P1′ group of the inhibitor for the TACE inhibitory activity. This work proves that these two classes of molecules could be used as potential leads for the development of TACE inhibitors.
