3-Indolyl sultams as selective CRTh2 antagonists

L. Nathan Tumey; Michael J. Robarge; Elizabeth Gleason; Jianping Song; Steven M. Murphy; George Ekema; Chris Doucette; Doug Hanniford; Marc Palmer; Gary Pawlowski; Joel Danzig; Margaret Loftus; Karen Hunady; Bruce Sherf; Robert W. Mays; Alain Stricker-Krongrad; Kurt R. Brunden; Youssef L. Bennani; John J. Harrington

doi:10.1016/j.bmcl.2010.04.046

3-Indolyl sultams as selective CRTh2 antagonists

L. Nathan Tumey
, Michael J. Robarge
, Elizabeth Gleason
, Jianping Song
, Steven M. Murphy
, George Ekema
, Chris Doucette
, Doug Hanniford
, Marc Palmer
, Gary Pawlowski
, Joel Danzig
, Margaret Loftus
, Karen Hunady
, Bruce Sherf
, Robert W. Mays
, Alain Stricker-Krongrad
, Kurt R. Brunden
, Youssef L. Bennani
, John J. Harrington

Pharmaceutical Sciences

Binghamton University

Athersys Ltd

Research output: Contribution to journal › Article › peer-review

46 Scopus citations

Abstract

CRTh2 (DP₂) is a prostaglandin D₂ receptor implicated in the recruitment of eosinophils and basophils within the asthmatic lung. Here we report the discovery of a novel series of 3-indolyl sultam antagonists with low nM affinity for CRTh2. These compounds proved to be selective over the other primary prostaglandin D₂ receptor (DP1) as well as the thromboxane A₂ receptor (TP).

Original language	English
Pages (from-to)	3287-3290
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	11
DOIs	https://doi.org/10.1016/j.bmcl.2010.04.046
State	Published - Jun 1 2010

Keywords

Antagonist
CRTh2
DP
Indole
Prostaglandin D2
Ramatroban
Sultam

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10.1016/j.bmcl.2010.04.046

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Tumey, L. N., Robarge, M. J., Gleason, E., Song, J., Murphy, S. M., Ekema, G., Doucette, C., Hanniford, D., Palmer, M., Pawlowski, G., Danzig, J., Loftus, M., Hunady, K., Sherf, B., Mays, R. W., Stricker-Krongrad, A., Brunden, K. R., Bennani, Y. L., & Harrington, J. J. (2010). 3-Indolyl sultams as selective CRTh2 antagonists. Bioorganic and Medicinal Chemistry Letters, 20(11), 3287-3290. https://doi.org/10.1016/j.bmcl.2010.04.046

@article{d5bb65fc8a0442759a6c846d1460ebd9,

title = "3-Indolyl sultams as selective CRTh2 antagonists",

abstract = "CRTh2 (DP2) is a prostaglandin D2 receptor implicated in the recruitment of eosinophils and basophils within the asthmatic lung. Here we report the discovery of a novel series of 3-indolyl sultam antagonists with low nM affinity for CRTh2. These compounds proved to be selective over the other primary prostaglandin D2 receptor (DP1) as well as the thromboxane A2 receptor (TP).",

keywords = "Antagonist, CRTh2, DP, Indole, Prostaglandin D2, Ramatroban, Sultam",

author = "Tumey, \{L. Nathan\} and Robarge, \{Michael J.\} and Elizabeth Gleason and Jianping Song and Murphy, \{Steven M.\} and George Ekema and Chris Doucette and Doug Hanniford and Marc Palmer and Gary Pawlowski and Joel Danzig and Margaret Loftus and Karen Hunady and Bruce Sherf and Mays, \{Robert W.\} and Alain Stricker-Krongrad and Brunden, \{Kurt R.\} and Bennani, \{Youssef L.\} and Harrington, \{John J.\}",

year = "2010",

month = jun,

day = "1",

doi = "10.1016/j.bmcl.2010.04.046",

language = "English",

volume = "20",

pages = "3287--3290",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

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Tumey, LN, Robarge, MJ, Gleason, E, Song, J, Murphy, SM, Ekema, G, Doucette, C, Hanniford, D, Palmer, M, Pawlowski, G, Danzig, J, Loftus, M, Hunady, K, Sherf, B, Mays, RW, Stricker-Krongrad, A, Brunden, KR, Bennani, YL & Harrington, JJ 2010, '3-Indolyl sultams as selective CRTh2 antagonists', Bioorganic and Medicinal Chemistry Letters, vol. 20, no. 11, pp. 3287-3290. https://doi.org/10.1016/j.bmcl.2010.04.046

TY - JOUR

T1 - 3-Indolyl sultams as selective CRTh2 antagonists

AU - Tumey, L. Nathan

AU - Robarge, Michael J.

AU - Gleason, Elizabeth

AU - Song, Jianping

AU - Murphy, Steven M.

AU - Ekema, George

AU - Doucette, Chris

AU - Hanniford, Doug

AU - Palmer, Marc

AU - Pawlowski, Gary

AU - Danzig, Joel

AU - Loftus, Margaret

AU - Hunady, Karen

AU - Sherf, Bruce

AU - Mays, Robert W.

AU - Stricker-Krongrad, Alain

AU - Brunden, Kurt R.

AU - Bennani, Youssef L.

AU - Harrington, John J.

PY - 2010/6/1

Y1 - 2010/6/1

N2 - CRTh2 (DP2) is a prostaglandin D2 receptor implicated in the recruitment of eosinophils and basophils within the asthmatic lung. Here we report the discovery of a novel series of 3-indolyl sultam antagonists with low nM affinity for CRTh2. These compounds proved to be selective over the other primary prostaglandin D2 receptor (DP1) as well as the thromboxane A2 receptor (TP).

AB - CRTh2 (DP2) is a prostaglandin D2 receptor implicated in the recruitment of eosinophils and basophils within the asthmatic lung. Here we report the discovery of a novel series of 3-indolyl sultam antagonists with low nM affinity for CRTh2. These compounds proved to be selective over the other primary prostaglandin D2 receptor (DP1) as well as the thromboxane A2 receptor (TP).

KW - Antagonist

KW - CRTh2

KW - DP

KW - Indole

KW - Prostaglandin D2

KW - Ramatroban

KW - Sultam

UR - https://www.scopus.com/pages/publications/77953292659

U2 - 10.1016/j.bmcl.2010.04.046

DO - 10.1016/j.bmcl.2010.04.046

M3 - Article

C2 - 20457519

SN - 0960-894X

VL - 20

SP - 3287

EP - 3290

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 11

ER -

3-Indolyl sultams as selective CRTh2 antagonists

Abstract

Keywords

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