论文信息 - Hit-to-Lead studies: the discovery of potent adamantane amide P2X7 receptor antagonists. - 字舞流文

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

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.

Martin Braddock | Keith Bowers | Richard Weaver | M. Braddock | R. Weaver | A. Baxter | T. Mcinally | M. Robertson | P. Webborn | Andrew Baxter | S. Brough | Steve Brough | Tom McInally | Janice Bent | Malbinder Fagura | Mandy Lawson | M. Mortimore | Mike Mortimore | Mark Robertson | Peter Webborn | M. Lawson | K. Bowers | M. Fagura | J. Bent

[1] F. Di Virgilio,et al. Synthesis and biological activity of N-arylpiperazine-modified analogues of KN-62, a potent antagonist of the purinergic P2X7 receptor. , 2003, Journal of medicinal chemistry.

[2] J. Wiley,et al. Adenosine triphosphate-induced shedding of CD23 and L-selectin (CD62L) from lymphocytes is mediated by the same receptor but different metalloproteases. , 1998, Blood.

[3] C. Gabel,et al. Interleukin-1 beta maturation and release in response to ATP and nigericin. Evidence that potassium depletion mediated by these agents is a necessary and common feature of their activity. , 1994, The Journal of biological chemistry.

[4] K. Jacobson,et al. Potent P2X7 receptor antagonists: Tyrosyl derivatives synthesized using a sequential parallel synthetic approach , 2001, Drug development research.

[5] C. Gabel,et al. Absence of the P2X7 Receptor Alters Leukocyte Function and Attenuates an Inflammatory Response , 2002, The Journal of Immunology.

[6] G. Burnstock,et al. Overview of P2 receptors: Possible functions in immune cells , 2001 .

[7] M. Mortimore,et al. The medicinal chemistry of the P2 receptor family. , 2001, Progress in medicinal chemistry.

[8] D. Ferrari,et al. On the Role of the P2X7 Receptor in the Immune System , 2001 .

[9] R. North. Molecular physiology of P2X receptors. , 2002, Physiological reviews.

[10] C. Gargett,et al. The isoquinoline derivative KN‐62 a potent antagonist of the P2Z‐receptor of human lymphocytes , 1997, British journal of pharmacology.