Neglected sulfur(vi) pharmacophores in drug discovery: exploration of novel chemical space by the interplay of drug design and method development (Dedicated to Professor Julius Rebek on the occasion of his 75th birthday.)

Historically, sulfoximines, sulfondiimines and sulfonimidamides have been neglected pharmacophores in drug discovery even though they offer very interesting properties. This highlight shares the key learnings of various lead optimization approaches at Bayer AG that have successfully utilized these n...

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Bibliographic Details
Published in:Organic chemistry frontiers an international journal of organic chemistry 2019-04, Vol.6 (8), p.1319-1324
Main Author: Lücking, U
Format: Article
Language:English
Subjects:
Drug development
Drug discovery
Functional groups
Historical account
Optimization
Organic chemistry
Pharmacology
PharmacoPhores
Sulfur
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Summary:Historically, sulfoximines, sulfondiimines and sulfonimidamides have been neglected pharmacophores in drug discovery even though they offer very interesting properties. This highlight shares the key learnings of various lead optimization approaches at Bayer AG that have successfully utilized these neglected sulfur(vi) functional groups to deliver multiple clinical candidates. In this context, the key synthetic methods utilized for the synthetic preparation of these unusual compounds will be outlined.
ISSN:2052-4110
2052-4110
DOI:10.1039/c8qo01233d