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Ring-Expansion Approach to Medium-Sized Lactams and Analysis of Their Medicinal Lead-Like Properties

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JournalChemistry : A European Journal
DateAccepted/In press - 9 Dec 2016
DateE-pub ahead of print - 18 Jan 2017
DatePublished (current) - 10 Feb 2017
Issue number9
Volume23
Number of pages6
Pages (from-to)2225-2230
Early online date18/01/17
Original languageEnglish

Abstract

Medium-sized rings are widely considered to be under-represented in biological screening libraries for lead identification in medicinal chemistry. To help address this, a library of medium-sized lactams has been generated by using a simple, scalable and versatile ring-expansion protocol. Analysis of the library by using open-access computational tool LLAMA suggested that these lactams and their derivatives have highly promising physicochemical and 3D spatial properties and thus have much potential in drug discovery.

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© 2017 Wiley-VCH Verlag GmbH & Co. This is an author-produced version of the published paper. Uploaded in accordance with the publisher’s self-archiving policy. Further copying may not be permitted; contact the publisher for details

    Research areas

  • amino acids, lactams, lead-oriented synthesis, medium-sized rings, ring expansion

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