排序方式: 共有2条查询结果,搜索用时 265 毫秒
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Jean-François Fournier Yushma Bhurruth-Alcor Branislav Musicki Jérome Aubert Michèle Aurelly Claire Bouix-Peter Karinne Bouquet Laurent Chantalat Marion Delorme Bénédicte Drean Gwenaelle Duvert Nicolas Fleury-Bregeot Blanche Gauthier Karine Grisendi Craig S. Harris Laurent F. Hennequin Tatiana Isabet Florence Joly Loïc Tomas 《Bioorganic & medicinal chemistry letters》2018,28(17):2985-2992
A series of squaramide-based hydroxamic acids were designed, synthesized and evaluated against human HDAC enzyme. Squaramides were found to be potent in the Hut78 cell line, but initially suffered from low solubility. Leads with improved solubility and metabolic profiles were shown to be class I, IIB and IV selective. 相似文献
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Jean-Guy Boiteau Gilles Ouvry Jean-Marie Arlabosse Stéphanie Astri Audrey Beillard Yushma Bhurruth-Alcor Laetitia Bonnary Claire Bouix-Peter Karine Bouquet Marilyne Bourotte Isabelle Cardinaud Catherine Comino Benoît Deprez Denis Duvert Angélique Féret Feriel Hacini-Rachinel Craig S. Harris Anne-Pascale Luzy Laurent F. Hennequin 《Bioorganic & medicinal chemistry》2018,26(4):945-956
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 26a. Starting from hits plagued with poor solubility or genotoxicity, 26a was identified through thorough multiparameter optimisation. Showing robust in vivo activity in an oxazolone-mediated inflammation model, the compound was selected for development. Following a polymorph screen, the hydrochloride salt was selected and the synthesis was efficiently developed to yield the API in 47% overall yield. 相似文献
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