Curse or Cure? A Perspective on the Developability of Aldehydes as Active Pharmaceutical Ingredients

There is a dichotomy between the increasing utility of aldehydes as tool molecules that bind to “undruggable” protein sites and the designation of the aldehyde functional group as a structural alert by the medicinal chemistry community. Herein we compile information about pharmacologically active al...

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Bibliographic Details
Published inJournal of medicinal chemistry Vol. 63; no. 23; pp. 14357 - 14381
Main Authors Gampe, Christian, Verma, Vishal A
Format Journal Article
LanguageEnglish
Published United States American Chemical Society 10.12.2020
Subjects
Aldehydes - chemistry
Aldehydes - pharmacology
Excipients - chemistry
Pharmaceutical Preparations - chemistry
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Summary:There is a dichotomy between the increasing utility of aldehydes as tool molecules that bind to “undruggable” protein sites and the designation of the aldehyde functional group as a structural alert by the medicinal chemistry community. Herein we compile information about pharmacologically active aldehydes that are being used in humans. We summarize the learnings from these data, discuss advantages and challenges associated with aldehydes, and derive strategies for the successful development of aldehydes within drug discovery programs.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
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content type line 23
ObjectType-Review-1
ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.0c01177