Literature DB >> 18240382

1-(2-Phenoxyphenyl)methanamines: SAR for dual serotonin/noradrenaline reuptake inhibition, metabolic stability and hERG affinity.

Gavin A Whitlock1, Julian Blagg, Paul V Fish.   

Abstract

A novel series of 1-(2-phenoxyphenyl)methanamines is disclosed, which possess selective dual 5-HT and NA reuptake pharmacology. Analogues with good human in vitro metabolic stability, hERG selectivity and passive membrane permeability were identified.

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Year:  2008        PMID： 18240382     DOI： 10.1016/j.bmcl.2007.11.080

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  3 in total

1.  Testing physical models of passive membrane permeation.

Authors:  Siegfried S F Leung; Jona Mijalkovic; Kenneth Borrelli; Matthew P Jacobson
Journal:  J Chem Inf Model       Date:  2012-05-24       Impact factor: 4.956

2.  Picomolar inhibitors of HIV reverse transcriptase featuring bicyclic replacement of a cyanovinylphenyl group.

Authors:  Won-Gil Lee; Ricardo Gallardo-Macias; Kathleen M Frey; Krasimir A Spasov; Mariela Bollini; Karen S Anderson; William L Jorgensen
Journal:  J Am Chem Soc       Date:  2013-10-24       Impact factor: 15.419

3.  Optimization of imidazo[4,5-b]pyridine-based kinase inhibitors: identification of a dual FLT3/Aurora kinase inhibitor as an orally bioavailable preclinical development candidate for the treatment of acute myeloid leukemia.

Authors:  Vassilios Bavetsias; Simon Crumpler; Chongbo Sun; Sian Avery; Butrus Atrash; Amir Faisal; Andrew S Moore; Magda Kosmopoulou; Nathan Brown; Peter W Sheldrake; Katherine Bush; Alan Henley; Gary Box; Melanie Valenti; Alexis de Haven Brandon; Florence I Raynaud; Paul Workman; Suzanne A Eccles; Richard Bayliss; Spiros Linardopoulos; Julian Blagg
Journal:  J Med Chem       Date:  2012-10-08       Impact factor: 7.446
  3 in total

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