File(s) not publicly available
Synthesis and biological evaluation of a library containing potentially 1600 amides / esters. A strategy for rapid compound generation and screening
journal contribution
posted on 2023-06-08, 19:32 authored by Paul W Smith, Justine Y Q Lai, Andrew R Whittington, Brian Cox, John G Houston, C Harri Stylli, Martyn N Banks, Philip R TillerA library of potentially 1600amide/ester dimers was prepared by reacting 40 acid chlorides with 40 nucleophiles. The whole library was presented for biological screening in 80 sample mixtures, with each of the possible products appearing in a unique pair of samples. The potential of this strategy for rapid identification of chemical leads was demostrated by the discovery of (1) with micromolar affinity for the NK3 receptor and (2), a weak inhibitor of the matrix metalloprotease MMP-1.
History
Publication status
- Published
Journal
Bioorganic and Medicinal Chemistry LettersISSN
0960-894XPublisher
ElsevierExternal DOI
Issue
24Volume
4Page range
2821-2824Department affiliated with
- Chemistry Publications
Full text available
- No
Peer reviewed?
- Yes
Legacy Posted Date
2015-01-14Usage metrics
Categories
No categories selectedKeywords
Licence
Exports
RefWorks
BibTeX
Ref. manager
Endnote
DataCite
NLM
DC