%0 Journal Article %1 Conti1998 %A Conti, P. %A Dallanoce, C. %A Amici, M. De %A Micheli, C. De %A Klotz, K. N. %D 1998 %J Bioorg Med Chem %K & Adenylate Adrenergic Animals Assay Binding, CHO Chromatography, Competitive Cricetinae Cultured Cyclase/metabolism Glioma Humans Isoxazoles/*chemical Layer Magnetic Pindolol/analogs Propanolamines/metabolism Radioligand Rats Resonance Spectroscopy Thin Tumor beta-1/*antagonists beta-2/*antagonists beta-Agonists/*chemical beta-Antagonists/*chemical derivatives/metabolism inhibitors/metabolism synthesis/metabolism Receptor Cell %N 4 %P 401-8 %T Synthesis of new delta 2-isoxazoline derivatives and their pharmacological characterization as beta-adrenergic receptor antagonists %U http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=9597184 %V 6 %X A series of delta 2-isoxazoline derivatives structurally related to Broxaterol 1 and Falintolol 3 has been prepared and evaluated for their binding affinity to beta 1- and beta 2-adrenergic receptors. Among the tested compounds only the 3-isopropenyl anti derivative 4d is as active as the reference compounds. An electron-releasing group, probably operating through a pi-pi interaction, in the 3-position of the isoxazoline nucleus greatly enhances the affinity of the compounds. Conversely, the closest analogs of Broxaterol (3-bromo delta 2-isoxazolines 4a and 5a) are at least one order of magnitude less active than the model compound 1. Throughout the series of derivatives the anti stereoisomers are invariably more active than their syn counterparts.

@article{Conti1998, abstract = {A series of delta 2-isoxazoline derivatives structurally related to Broxaterol 1 and Falintolol 3 has been prepared and evaluated for their binding affinity to beta 1- and beta 2-adrenergic receptors. Among the tested compounds only the 3-isopropenyl anti derivative 4d is as active as the reference compounds. An electron-releasing group, probably operating through a pi-pi interaction, in the 3-position of the isoxazoline nucleus greatly enhances the affinity of the compounds. Conversely, the closest analogs of Broxaterol (3-bromo delta 2-isoxazolines 4a and 5a) are at least one order of magnitude less active than the model compound 1. Throughout the series of derivatives the anti stereoisomers are invariably more active than their syn counterparts.}, added-at = {2010-12-14T18:12:02.000+0100}, author = {Conti, P. and Dallanoce, C. and Amici, M. De and Micheli, C. De and Klotz, K. N.}, biburl = {https://www.bibsonomy.org/bibtex/296ddf401b33efc46c0d10e94690703e8/pharmawuerz}, endnotereftype = {Journal Article}, interhash = {370b02c9507ead2a5c9358ac180e74cc}, intrahash = {96ddf401b33efc46c0d10e94690703e8}, issn = {0968-0896 (Print) 0968-0896 (Linking)}, journal = {Bioorg Med Chem}, keywords = {& Adenylate Adrenergic Animals Assay Binding, CHO Chromatography, Competitive Cricetinae Cultured Cyclase/metabolism Glioma Humans Isoxazoles/*chemical Layer Magnetic Pindolol/analogs Propanolamines/metabolism Radioligand Rats Resonance Spectroscopy Thin Tumor beta-1/*antagonists beta-2/*antagonists beta-Agonists/*chemical beta-Antagonists/*chemical derivatives/metabolism inhibitors/metabolism synthesis/metabolism Receptor Cell}, month = Apr, note = {Conti, P Dallanoce, C De Amici, M De Micheli, C Klotz, K N Research Support, Non-U.S. Gov't England Bioorganic \& medicinal chemistry Bioorg Med Chem. 1998 Apr;6(4):401-8.}, number = 4, pages = {401-8}, shorttitle = {Synthesis of new delta 2-isoxazoline derivatives and their pharmacological characterization as beta-adrenergic receptor antagonists}, timestamp = {2010-12-14T18:22:39.000+0100}, title = {Synthesis of new delta 2-isoxazoline derivatives and their pharmacological characterization as beta-adrenergic receptor antagonists}, url = {http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=9597184}, volume = 6, year = 1998 }