38486-01-0Relevant articles and documents
Coumarins and adenosine receptors: New perceptions in structure–affinity relationships
Fonseca, André,Matos, Maria Jo?o,Vilar, Santiago,Kachler, Sonja,Klotz, Karl-Norbert,Uriarte, Eugenio,Borges, Fernanda
, p. 245 - 256 (2017/12/29)
Adenosine receptor (AR) subtypes are involved in several physiological and pharmacological processes. Ligands that are able to selectively modulate one receptor subtype can delay or slow down the progression of diverse diseases. In this context, our research group focused its investigation into the discovery and development of novel, potent and selective AR ligands based on coumarin scaffold. Therefore, a series of 3-phenylcarboxamidocoumarins were synthesized and their affinity for the human AR subtypes was screened by radioligand binding assays for A1, A2A and A3 receptors and for A2B by adenylyl cyclase assay. Compound 26 was found to be the most remarkable, with a hA1/hA3 and hA2A/hA3 selectivity of 42, for the A3 AR (Ki?=?2.4?μm). Receptor-driven molecular modelling studies have provided valuable information on the binding/selectivity data of compound 26 and for the following optimization process. Moreover, compound 26 presents drug-like properties according to the general guidelines linked to the concept.
Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors
Robert, Séverine,Bertolla, Carine,Masereel, Bernard,Dogné, Jean-Michel,Pochet, Lionel
supporting information; experimental part, p. 3077 - 3080 (2009/04/07)
Recently, FXIIa was highlighted as an original attractive target for the development of new anticoagulant drugs with low rates of therapy-related hemorrhages. In this work, we describe the development of a new series of 3-carboxamide-coumarins that are the first potent and selective nonpeptidic inhibitors of FXIIa.
