An article 2-Phenyloxazole-4-carboxamide as a Scaffold for Selective Inhibition of Human Monoamine Oxidase B WOS:000481206700001 published article about MAO INHIBITORS; PROTEIN; DISCOVERY; DERIVATIVES; DOCKING; ANALOGS; TARGET; POTENT; CELLS; PC12 in [Dalla Via, Lisa] Univ Padua, Dipartimento Sci Farmaco, Via F Marzolo 5, I-35131 Padua, Italy; [Di Paolo, Maria L.] Univ Padua, Dipartimento Med Mol, Via G Colombo 3, I-35131 Padua, Italy; [Christodoulou, Michael S.] Univ Milan, DISFARM, Sez Chim Gen & Organ A Marchesini, Via Venezian 21, I-20133 Milan, Italy; [Calogero, Alessandra M.; Cappelletti, Graziella] Univ Milan, Dipartimento Biosci, Via Celoria 26, I-20133 Milan, Italy; [Pinzi, Luca; Rastelli, Giulio] Univ Modena & Reggio Emilia, Dipartimento Sci Vita, Via Campi 103, I-41125 Modena, Italy; [Passarella, Daniele] Univ Milan, Dipartimento Chim, Via C Golgi 19, I-20133 Milan, Italy in 2019.0, Cited 70.0. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9. Formula: C13H13N
A series of 2-phenyloxazoles bearing an amide group at position 4 were designed and synthesized for evaluation as potential inhibitors of human recombinant monoamine oxidases (hrMAOs). Results of kinetics experiments demonstrated that all compounds behave as competitive MAO inhibitors, with good selectivity toward the MAO-B isoform. The most potent and selective derivatives are characterized by inhibition constant (K-i) values in the sub-micromolar range and a good selectivity index (Ki MAO-A/Ki MAO-B>50). Some derivatives were also found to be able to inhibit MAO activity in nerve growth factor (NGF)-differentiated PC12 cells, taken as a model of neuronal cells. In particular, 2-(2-hydroxyphenyl)-N-phenyloxazole-4-carboxamide (compound 4 a) may be a promising new scaffold, exerting the highest selectivity and inhibitory effect toward MAOs in NGF-differentiated PC12 cell lysates, without compromising cell viability. Molecular docking analysis allowed a rationalization of the experimentally observed binding affinity and selectivity.
Formula: C13H13N. About Diphenylmethanamine, If you have any questions, you can contact Di Paolo, ML; Christodoulou, MS; Calogero, AM; Pinzi, L; Rastelli, G; Passarella, D; Cappelletti, G; Dalla Via, L or concate me.
Reference:
Amide – Wikipedia,
,Amide – an overview | ScienceDirect Topics