Variously substituted N-aryl-4-oxo-4H-chromene-3-carboxamide derivatives present planar conformations between the carboxamide moiety and the chromone ring stabilized by intramolecular N-H O hydrogen bonding. Despite the similarity in structures, they function differentially as h-MAO-B inhibitors, an observation correlated with the electronic moderation induced by the substituents in the exocyclic aryl ring.
See: Gomes, Low, Cagide, Chavarria & Borges[Acta Cryst. (2015). E71, 547-554]. https://journals.iucr.org/e/issues/2015/05/00/
The crystal structures of four N-(4-halophenyl)-4-oxo-4H-chromene-3-carboxamides (halo = F, Cl, Br and I) are described. Each molecule features intramolecular N-H…O and C-H…O hydrogen bonds, which help to establish a near planar conformation. This may correlate with their promising monoamino oxidase inhibitor activity, which could lead to new insights into possible treatments of Parkinson’s disease.
See: Gomes, Low, Cagide & Borges [Acta Cryst. (2014). E70, 88-93]. http://journals.iucr.org/e/issues/2015/01/00/
Back Cover illustration
The back cover picture shows 3‐arylcoumarin analogues targeting A1, A2A, A2B and A3 adenosine receptors (ARs). At the cellular level, most of the compounds proved to be selective A3 AR ligands, which makes them promising development candidates for the treatment of asthma, inflammatory and neurodegenerative diseases, and as protective agents against cardiac ischemia.
See: [ChemMedChem.. 2014 Jul 18. DOI: 10.1002/cmdc.201402205] https://onlinelibrary.wiley.com/doi/10.1002/cmdc.201490039