Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists

Koc Kan Ho; Douglas S. Auld; Adolph C. Bohnstedt; Paolo Conti; Wim Dokter; Shawn Erickson; Daming Feng; Jim Inglese; Celia Kingsbury; Steven G. Kultgen; Rong Qiang Liu; Christopher M. Masterson; Michael Ohlmeyer; Yajing Rong; Martijn Rooseboom; Andrew Roughton; Philippe Samama; Martin Jan Smit; Ellen Son; Jaap van der Louw; Gerard Vogel; Maria Webb; Jac Wijkmans; Ming You

doi:10.1016/j.bmcl.2006.02.028

Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists

Koc Kan Ho, Douglas S. Auld, Adolph C. Bohnstedt, Paolo Conti, Wim Dokter, Shawn Erickson, Daming Feng, Jim Inglese, Celia Kingsbury, Steven G. Kultgen, Rong Qiang Liu, Christopher M. Masterson, Michael Ohlmeyer, Yajing Rong, Martijn Rooseboom, Andrew Roughton, Philippe Samama, Martin Jan Smit, Ellen Son, Jaap van der LouwGerard Vogel, Maria Webb, Jac Wijkmans, Ming You

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

28 Scopus citations

Abstract

An imidazolylpyrimidine was identified in a CXCR2 chemokine receptor antagonist screen and was optimized for potency, in vitro metabolic stability, and oral bioavailability. It was found that subtle structural modification within the series affected the oral bioavailability. Potent and orally available CXCR2 antagonists are herein reported.

Original language	English
Pages (from-to)	2724-2728
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	10
DOIs	https://doi.org/10.1016/j.bmcl.2006.02.028
State	Published - 15 May 2006
Externally published	Yes

Keywords

CXCR2
Chemokine
Microsomal stability
Oral bioavailability
Pyrimidine

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10.1016/j.bmcl.2006.02.028

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Ho, K. K., Auld, D. S., Bohnstedt, A. C., Conti, P., Dokter, W., Erickson, S., Feng, D., Inglese, J., Kingsbury, C., Kultgen, S. G., Liu, R. Q., Masterson, C. M., Ohlmeyer, M., Rong, Y., Rooseboom, M., Roughton, A., Samama, P., Smit, M. J., Son, E., ... You, M. (2006). Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists. Bioorganic and Medicinal Chemistry Letters, 16(10), 2724-2728. https://doi.org/10.1016/j.bmcl.2006.02.028

@article{39fce266e07141cd8c37832015f817a2,

title = "Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists",

abstract = "An imidazolylpyrimidine was identified in a CXCR2 chemokine receptor antagonist screen and was optimized for potency, in vitro metabolic stability, and oral bioavailability. It was found that subtle structural modification within the series affected the oral bioavailability. Potent and orally available CXCR2 antagonists are herein reported.",

keywords = "CXCR2, Chemokine, Microsomal stability, Oral bioavailability, Pyrimidine",

author = "Ho, {Koc Kan} and Auld, {Douglas S.} and Bohnstedt, {Adolph C.} and Paolo Conti and Wim Dokter and Shawn Erickson and Daming Feng and Jim Inglese and Celia Kingsbury and Kultgen, {Steven G.} and Liu, {Rong Qiang} and Masterson, {Christopher M.} and Michael Ohlmeyer and Yajing Rong and Martijn Rooseboom and Andrew Roughton and Philippe Samama and Smit, {Martin Jan} and Ellen Son and {van der Louw}, Jaap and Gerard Vogel and Maria Webb and Jac Wijkmans and Ming You",

year = "2006",

month = may,

day = "15",

doi = "10.1016/j.bmcl.2006.02.028",

language = "English",

volume = "16",

pages = "2724--2728",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd.",

number = "10",

}

Ho, KK, Auld, DS, Bohnstedt, AC, Conti, P, Dokter, W, Erickson, S, Feng, D, Inglese, J, Kingsbury, C, Kultgen, SG, Liu, RQ, Masterson, CM, Ohlmeyer, M, Rong, Y, Rooseboom, M, Roughton, A, Samama, P, Smit, MJ, Son, E, van der Louw, J, Vogel, G, Webb, M, Wijkmans, J & You, M 2006, 'Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists', Bioorganic and Medicinal Chemistry Letters, vol. 16, no. 10, pp. 2724-2728. https://doi.org/10.1016/j.bmcl.2006.02.028

TY - JOUR

T1 - Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists

AU - Ho, Koc Kan

AU - Auld, Douglas S.

AU - Bohnstedt, Adolph C.

AU - Conti, Paolo

AU - Dokter, Wim

AU - Erickson, Shawn

AU - Feng, Daming

AU - Inglese, Jim

AU - Kingsbury, Celia

AU - Kultgen, Steven G.

AU - Liu, Rong Qiang

AU - Masterson, Christopher M.

AU - Ohlmeyer, Michael

AU - Rong, Yajing

AU - Rooseboom, Martijn

AU - Roughton, Andrew

AU - Samama, Philippe

AU - Smit, Martin Jan

AU - Son, Ellen

AU - van der Louw, Jaap

AU - Vogel, Gerard

AU - Webb, Maria

AU - Wijkmans, Jac

AU - You, Ming

PY - 2006/5/15

Y1 - 2006/5/15

N2 - An imidazolylpyrimidine was identified in a CXCR2 chemokine receptor antagonist screen and was optimized for potency, in vitro metabolic stability, and oral bioavailability. It was found that subtle structural modification within the series affected the oral bioavailability. Potent and orally available CXCR2 antagonists are herein reported.

AB - An imidazolylpyrimidine was identified in a CXCR2 chemokine receptor antagonist screen and was optimized for potency, in vitro metabolic stability, and oral bioavailability. It was found that subtle structural modification within the series affected the oral bioavailability. Potent and orally available CXCR2 antagonists are herein reported.

KW - CXCR2

KW - Chemokine

KW - Microsomal stability

KW - Oral bioavailability

KW - Pyrimidine

UR - http://www.scopus.com/inward/record.url?scp=33645885315&partnerID=8YFLogxK

U2 - 10.1016/j.bmcl.2006.02.028

DO - 10.1016/j.bmcl.2006.02.028

M3 - Article

C2 - 16540318

AN - SCOPUS:33645885315

SN - 0960-894X

VL - 16

SP - 2724

EP - 2728

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 10

ER -

Imidazolylpyrimidine based CXCR2 chemokine receptor antagonists

Abstract

Keywords

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