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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 Tiller
A 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 Letters

ISSN

0960-894X

Publisher

Elsevier

Issue

24

Volume

4

Page range

2821-2824

Department affiliated with

  • Chemistry Publications

Full text available

  • No

Peer reviewed?

  • Yes

Legacy Posted Date

2015-01-14

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