Design and synthesis of novel CCR2 antagonists: Investigation of non-aryl/heteroaryl binding motifs
JOHN L. TRUJILLO
1
,
Wei Huang
1
,
Robert O Hughes
1
,
D Joseph Rogier
1
,
Steven R Turner
1
,
Rajesh Devraj
1
,
Philip A. Morton
2
,
Chu-Biao Xue
3
,
Ganfeng Chao
3
,
Maryanne B. Covington
4
,
Robert Newton
4
,
Brian Metcalf
3
1
Department of Medicinal Chemistry, Pfizer Global Research and Development, Chesterfield, MO 63017, USA
|
2
Department of Biochemical Pharmacology, Pfizer Global Research and Development, Chesterfield, MO 63017, USA
|
3
Department of Medicinal Chemistry, Incyte Corporation, Wilmington, DE, USA
|
4
Department of Biochemstry/Enzymology, Incyte Corporation, Wilmington, DE, USA
|
Тип публикации: Journal Article
Дата публикации: 2011-03-01
scimago Q2
wos Q2
БС2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
21316220
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Краткое описание
This report describes the design and synthesis of a series of CCR2 antagonists incorporating novel non-aryl/heteroaryl RHS (right hand side) motifs. Previous SAR in the area has suggested an aryl/heteroaryl substituent as a necessary structural feature for binding to the CCR2 receptor. Herein we describe the SAR with regards to potency (binding to hCCR2), dofetilide activity and metabolic stability (in vitro HLM) for this series. The resulting outcome was the identification of compounds with excellent properties for the investigation of the role of CCR2 in disease.
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TRUJILLO J. L. et al. Design and synthesis of novel CCR2 antagonists: Investigation of non-aryl/heteroaryl binding motifs // Bioorganic and Medicinal Chemistry Letters. 2011. Vol. 21. No. 6. pp. 1827-1831.
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TRUJILLO J. L., Huang W., Hughes R. O., Joseph Rogier D., Turner S. R., Devraj R., Morton P. A., Xue C., Chao G., Covington M. B., Newton R., Metcalf B. Design and synthesis of novel CCR2 antagonists: Investigation of non-aryl/heteroaryl binding motifs // Bioorganic and Medicinal Chemistry Letters. 2011. Vol. 21. No. 6. pp. 1827-1831.
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TY - JOUR
DO - 10.1016/j.bmcl.2011.01.052
UR - https://doi.org/10.1016/j.bmcl.2011.01.052
TI - Design and synthesis of novel CCR2 antagonists: Investigation of non-aryl/heteroaryl binding motifs
T2 - Bioorganic and Medicinal Chemistry Letters
AU - TRUJILLO, JOHN L.
AU - Huang, Wei
AU - Hughes, Robert O
AU - Joseph Rogier, D
AU - Turner, Steven R
AU - Devraj, Rajesh
AU - Morton, Philip A.
AU - Xue, Chu-Biao
AU - Chao, Ganfeng
AU - Covington, Maryanne B.
AU - Newton, Robert
AU - Metcalf, Brian
PY - 2011
DA - 2011/03/01
PB - Elsevier
SP - 1827-1831
IS - 6
VL - 21
PMID - 21316220
SN - 0960-894X
SN - 1464-3405
ER -
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@article{2011_TRUJILLO,
author = {JOHN L. TRUJILLO and Wei Huang and Robert O Hughes and D Joseph Rogier and Steven R Turner and Rajesh Devraj and Philip A. Morton and Chu-Biao Xue and Ganfeng Chao and Maryanne B. Covington and Robert Newton and Brian Metcalf},
title = {Design and synthesis of novel CCR2 antagonists: Investigation of non-aryl/heteroaryl binding motifs},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2011},
volume = {21},
publisher = {Elsevier},
month = {mar},
url = {https://doi.org/10.1016/j.bmcl.2011.01.052},
number = {6},
pages = {1827--1831},
doi = {10.1016/j.bmcl.2011.01.052}
}
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MLA
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TRUJILLO, JOHN L., et al. “Design and synthesis of novel CCR2 antagonists: Investigation of non-aryl/heteroaryl binding motifs.” Bioorganic and Medicinal Chemistry Letters, vol. 21, no. 6, Mar. 2011, pp. 1827-1831. https://doi.org/10.1016/j.bmcl.2011.01.052.