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Ring‐Expansion Approach to Medium‐Sized Lactams and Analysis of Their Medicinal Lead‐Like Properties
Author(s) -
Baud Laetitia G.,
Manning Morgan A.,
Arkless Helen L.,
Stephens Thomas C.,
Unsworth William P.
Publication year - 2017
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201605615
Subject(s) - drug discovery , ring (chemistry) , lead (geology) , combinatorial chemistry , computer science , identification (biology) , nanotechnology , chemistry , materials science , biology , organic chemistry , biochemistry , paleontology , botany
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.