Synthesis and Biological Evaluation of New 2-(4,5-Dihydro-1H-imidazol-2-yl)-3,4-dihydro-2H-1,4-benzoxazine Derivatives

• DOI: 10.1021/jm021050c
• Publication Date: 2003-05-01T04:25:55Z
• Authors: Frédérique Touzeau; Axelle Arrault; Gérald Guillaumet; Elizabeth Scalbert; Bruno Pfeiffer; Marie-Claire Rettori; Pierre Renard; Jean-Yves Mérour
• Keywords: Imidazoline receptor; Moiety; Ethylene diamine; Nitrogen atom; Affinities; Binding affinities; Absolute Configuration

2-(4,5-Dihydro-1H-imidazol-2-yl)-3,4-dihydro-2H-1,4-benzoxazine derivatives and tricyclic analogues with a fused additional ring on the nitrogen atom of benzoxazine moiety have been prepared evaluated for their cardiovascular effects as potential antihypertensive agents. The imidazoline was generated by reaction corresponding ethyl ester ethylenediamine. Affinities binding sites (IBS) I1 I2 α1 α2 adrenergic receptors were well mean arterial blood pressure (MAP) heart rate (HR) spontaneously hypertensive rats. With few exceptions most active compounds MAP those high affinities IBS receptor. Among these, compound 4h interesting is now, together its enantiomers, under complementary pharmacological evaluation.