Synthesis and biological evaluation of biphenyl amides that modulate the US28 receptor

Kralj A, Kurt E, Tschammer N, Heinrich M (2014)


Publication Status: Published

Publication Type: Journal article, Original article

Publication year: 2014

Journal

Book Volume: 9

Pages Range: 151-168

Journal Issue: 1

DOI: 10.1002/cmdc.201300369

Abstract

To prepare and biologically evaluate 38 new potential US28 allosteric modulators, we employed a straightforward synthetic route involving radical arylation. The study was based on a former lead structure but with the dihydroisoquinolinone moiety replaced by substituted biphenyls. The investigation of structure-activity relationships among the new biphenyl-derived ligands led to a preliminary pharmacophore model and the discovery of four promising candidates with full inverse agonist properties. Hit HCMV GPCRs ASAP! Employing a straightforward synthetic access involving radical arylation, 38 new potential US28 allosteric modulators were prepared and biologically evaluated. The investigation of structure-activity relationships among the new biphenyl-derived ligands led to a consistent model and the discovery of four promising candidates with full inverse agonist properties. Copyright © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

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How to cite

APA:

Kralj, A., Kurt, E., Tschammer, N., & Heinrich, M. (2014). Synthesis and biological evaluation of biphenyl amides that modulate the US28 receptor. ChemMedChem, 9(1), 151-168. https://dx.doi.org/10.1002/cmdc.201300369

MLA:

Kralj, Ana, et al. "Synthesis and biological evaluation of biphenyl amides that modulate the US28 receptor." ChemMedChem 9.1 (2014): 151-168.

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