Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas

Jian Jin; Yonghui Wang; Dongchuan Shi; Feng Wang; Wei Fu; Roderick S. Davis; Qi Jin; James J. Foley; Henry M. Sarau; Dwight M. Morrow; Michael L. Moore; Ralph A. Rivero; Michael Palovich; Michael Salmon; Kristen E. Belmonte; Jakob Busch-Petersen

doi:10.1016/j.bmcl.2008.09.020

Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas

Jian Jin
, Yonghui Wang
, Dongchuan Shi
, Feng Wang
, Wei Fu
, Roderick S. Davis
, Qi Jin
, James J. Foley
, Henry M. Sarau
, Dwight M. Morrow
, Michael L. Moore
, Ralph A. Rivero
, Michael Palovich
, Michael Salmon
, Kristen E. Belmonte
, Jakob Busch-Petersen

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

4 Scopus citations

Abstract

SAR exploration of multiple regions of a tyrosine urea template led to the identification of very potent muscarinic acetylcholine receptor antagonists such as 10b with good subtype selectivity for M₃ over M₁. The structure-activity relationships (SAR) and optimization of the tyrosine urea series are described.

Original language	English
Pages (from-to)	5481-5486
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	18
Issue number	20
DOIs	https://doi.org/10.1016/j.bmcl.2008.09.020
State	Published - 15 Oct 2008
Externally published	Yes

Keywords

Asthma
COPD
M3 mAChR
Muscarinic acetylcholine receptor antagonists
SAR
Subtype selectivity
Tyrosine ureas

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10.1016/j.bmcl.2008.09.020

Cite this

Jin, J., Wang, Y., Shi, D., Wang, F., Fu, W., Davis, R. S., Jin, Q., Foley, J. J., Sarau, H. M., Morrow, D. M., Moore, M. L., Rivero, R. A., Palovich, M., Salmon, M., Belmonte, K. E., & Busch-Petersen, J. (2008). Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas. Bioorganic and Medicinal Chemistry Letters, 18(20), 5481-5486. https://doi.org/10.1016/j.bmcl.2008.09.020

@article{19617b54bbd344bd903b68165e707b3c,

title = "Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas",

abstract = "SAR exploration of multiple regions of a tyrosine urea template led to the identification of very potent muscarinic acetylcholine receptor antagonists such as 10b with good subtype selectivity for M3 over M1. The structure-activity relationships (SAR) and optimization of the tyrosine urea series are described.",

keywords = "Asthma, COPD, M3 mAChR, Muscarinic acetylcholine receptor antagonists, SAR, Subtype selectivity, Tyrosine ureas",

author = "Jian Jin and Yonghui Wang and Dongchuan Shi and Feng Wang and Wei Fu and Davis, \{Roderick S.\} and Qi Jin and Foley, \{James J.\} and Sarau, \{Henry M.\} and Morrow, \{Dwight M.\} and Moore, \{Michael L.\} and Rivero, \{Ralph A.\} and Michael Palovich and Michael Salmon and Belmonte, \{Kristen E.\} and Jakob Busch-Petersen",

year = "2008",

month = oct,

day = "15",

doi = "10.1016/j.bmcl.2008.09.020",

language = "English",

volume = "18",

pages = "5481--5486",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd.",

number = "20",

}

Jin, J, Wang, Y, Shi, D, Wang, F, Fu, W, Davis, RS, Jin, Q, Foley, JJ, Sarau, HM, Morrow, DM, Moore, ML, Rivero, RA, Palovich, M, Salmon, M, Belmonte, KE & Busch-Petersen, J 2008, 'Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas', Bioorganic and Medicinal Chemistry Letters, vol. 18, no. 20, pp. 5481-5486. https://doi.org/10.1016/j.bmcl.2008.09.020

TY - JOUR

T1 - Muscarinic acetylcholine receptor antagonists

T2 - SAR and optimization of tyrosine ureas

AU - Jin, Jian

AU - Wang, Yonghui

AU - Shi, Dongchuan

AU - Wang, Feng

AU - Fu, Wei

AU - Davis, Roderick S.

AU - Jin, Qi

AU - Foley, James J.

AU - Sarau, Henry M.

AU - Morrow, Dwight M.

AU - Moore, Michael L.

AU - Rivero, Ralph A.

AU - Palovich, Michael

AU - Salmon, Michael

AU - Belmonte, Kristen E.

AU - Busch-Petersen, Jakob

PY - 2008/10/15

Y1 - 2008/10/15

N2 - SAR exploration of multiple regions of a tyrosine urea template led to the identification of very potent muscarinic acetylcholine receptor antagonists such as 10b with good subtype selectivity for M3 over M1. The structure-activity relationships (SAR) and optimization of the tyrosine urea series are described.

AB - SAR exploration of multiple regions of a tyrosine urea template led to the identification of very potent muscarinic acetylcholine receptor antagonists such as 10b with good subtype selectivity for M3 over M1. The structure-activity relationships (SAR) and optimization of the tyrosine urea series are described.

KW - Asthma

KW - COPD

KW - M3 mAChR

KW - Muscarinic acetylcholine receptor antagonists

KW - SAR

KW - Subtype selectivity

KW - Tyrosine ureas

UR - https://www.scopus.com/pages/publications/53349166981

U2 - 10.1016/j.bmcl.2008.09.020

DO - 10.1016/j.bmcl.2008.09.020

M3 - Article

C2 - 18818072

AN - SCOPUS:53349166981

SN - 0960-894X

VL - 18

SP - 5481

EP - 5486

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 20

ER -

Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas

Abstract

Keywords

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