Hit-to-Lead studies: the discovery of potent adamantane amide P2X7 receptor antagonists

Andrew Baxter; Janice Bent; Keith Bowers; Martin Braddock; Steve Brough; Malbinder Fagura; Mandy Lawson; Tom McInally; Mike Mortimore; Mark Robertson; Richard Weaver; Peter Webborn

doi:10.1016/j.bmcl.2003.08.034

Hit-to-Lead studies: the discovery of potent adamantane amide P2X7 receptor antagonists

Bioorg Med Chem Lett. 2003 Nov 17;13(22):4047-50. doi: 10.1016/j.bmcl.2003.08.034.

Authors

Andrew Baxter¹, Janice Bent, Keith Bowers, Martin Braddock, Steve Brough, Malbinder Fagura, Mandy Lawson, Tom McInally, Mike Mortimore, Mark Robertson, Richard Weaver, Peter Webborn

Affiliation

¹ AstraZeneca R&D Charnwood, Bakewell Road, Loughborough LE11 5RH, UK. andrew.jg.baxter@astrazeneca.com

PMID: 14592505
DOI: 10.1016/j.bmcl.2003.08.034

Abstract

A Hit-to-Lead optimisation programme was carried out on the adamantane high throughput screening hit 1 resulting in the discovery of a number of potent P2X(7) antagonists.

Publication types

Comparative Study

MeSH terms

Adamantane / analogs & derivatives*
Adamantane / chemical synthesis
Adamantane / pharmacology*
Amides / chemical synthesis
Amides / pharmacology*
Drug Design
Humans
Kinetics
Purinergic P2 Receptor Antagonists*
Receptors, Purinergic P2X7
Structure-Activity Relationship

Substances

Amides
P2RX7 protein, human
Purinergic P2 Receptor Antagonists
Receptors, Purinergic P2X7
Adamantane