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An efficient asymmetric synthesis of the potent beta-blocker ICI-118,551 allows the determination of enantiomer dependency on biological activity

Baker, JR; Hothersall, JD; Fitzmaurice, RJ; Tucknott, M; Vinter, A; Tinker, A; Caddick, S; (2010) An efficient asymmetric synthesis of the potent beta-blocker ICI-118,551 allows the determination of enantiomer dependency on biological activity. CHEM COMMUN , 46 (22) 3953 - 3954. 10.1039/c0cc00142b.

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Abstract

A highly efficient, practical and. flexible two-step asymmetric synthesis of the beta(2)-selective beta-blocker ICI 118,551 is reported, allowing an unambiguous determination of the dependency of biological activity with optical activity, revealing the S,S-enantiomer to be the most potent.

Type:Article
Title:An efficient asymmetric synthesis of the potent beta-blocker ICI-118,551 allows the determination of enantiomer dependency on biological activity
DOI:10.1039/c0cc00142b
Keywords:PROTEIN-COUPLED RECEPTOR, CRYSTAL-STRUCTURE, RESOLUTION, SELECTIVITY, EPOXIDATION, ANTAGONISTS
UCL classification:UCL > School of Life and Medical Sciences > Faculty of Medical Sciences > Medicine (Division of)
UCL > School of BEAMS > Faculty of Maths and Physical Sciences > Chemistry
UCL > VP Enterprise

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