Discovery of novel and long acting muscarinic acetylcholine receptor antagonists

Jian Jin; Yonghui Wang; Dongchuan Shi; Feng Wang; Roderick S. Davis; Qi Jin; Wei Fu; James J. Foley; Edward F. Webb; Chris J. Dehaas; Manuela Berlanga; Miriam Burman; Henry M. Sarau; Dwight M. Morrow; Parvathi Rao; Lorena A. Kallal; Michael L. Moore; Ralph A. Rivero; Michael Palovich; Michael Salmon; Kristen E. Belmonte; Jakob Busch-Petersen

doi:10.1021/jm800634k

Discovery of novel and long acting muscarinic acetylcholine receptor antagonists

Jian Jin, Yonghui Wang, Dongchuan Shi, Feng Wang, Roderick S. Davis, Qi Jin, Wei Fu, James J. Foley, Edward F. Webb, Chris J. Dehaas, Manuela Berlanga, Miriam Burman, Henry M. Sarau, Dwight M. Morrow, Parvathi Rao, Lorena A. Kallal, Michael L. Moore, Ralph A. Rivero, Michael Palovich, Michael SalmonKristen E. Belmonte, Jakob Busch-Petersen

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

17 Scopus citations

Abstract

High throughput screening and subsequent optimization led to the discovery of novel quaternary ammonium salts as highly potent muscarinic acetylcholine receptor antagonists with excellent selectivity. Compounds 8a, 13a, and 13b showed excellent inhibitory activity and long duration of action in bronchoconstriction in vivo models in two species via intranasal or intratracheal administration. The novel inhaled muscarinic receptor antagonists are potentially useful therapeutic agents for the treatment of chronic obstructive pulmonary disease and other bronchoconstriction disorders.

Original language	English
Pages (from-to)	4866-4869
Number of pages	4
Journal	Journal of Medicinal Chemistry
Volume	51
Issue number	16
DOIs	https://doi.org/10.1021/jm800634k
State	Published - 28 Aug 2008
Externally published	Yes

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Jin, J., Wang, Y., Shi, D., Wang, F., Davis, R. S., Jin, Q., Fu, W., Foley, J. J., Webb, E. F., Dehaas, C. J., Berlanga, M., Burman, M., Sarau, H. M., Morrow, D. M., Rao, P., Kallal, L. A., Moore, M. L., Rivero, R. A., Palovich, M., ... Busch-Petersen, J. (2008). Discovery of novel and long acting muscarinic acetylcholine receptor antagonists. Journal of Medicinal Chemistry, 51(16), 4866-4869. https://doi.org/10.1021/jm800634k

@article{93b70af398eb4a76b36a59fbe80e2dad,

title = "Discovery of novel and long acting muscarinic acetylcholine receptor antagonists",

abstract = "High throughput screening and subsequent optimization led to the discovery of novel quaternary ammonium salts as highly potent muscarinic acetylcholine receptor antagonists with excellent selectivity. Compounds 8a, 13a, and 13b showed excellent inhibitory activity and long duration of action in bronchoconstriction in vivo models in two species via intranasal or intratracheal administration. The novel inhaled muscarinic receptor antagonists are potentially useful therapeutic agents for the treatment of chronic obstructive pulmonary disease and other bronchoconstriction disorders.",

author = "Jian Jin and Yonghui Wang and Dongchuan Shi and Feng Wang and Davis, {Roderick S.} and Qi Jin and Wei Fu and Foley, {James J.} and Webb, {Edward F.} and Dehaas, {Chris J.} and Manuela Berlanga and Miriam Burman and Sarau, {Henry M.} and Morrow, {Dwight M.} and Parvathi Rao and Kallal, {Lorena A.} 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 = aug,

day = "28",

doi = "10.1021/jm800634k",

language = "English",

volume = "51",

pages = "4866--4869",

journal = "Journal of Medicinal Chemistry",

issn = "0022-2623",

publisher = "American Chemical Society",

number = "16",

}

Jin, J, Wang, Y, Shi, D, Wang, F, Davis, RS, Jin, Q, Fu, W, Foley, JJ, Webb, EF, Dehaas, CJ, Berlanga, M, Burman, M, Sarau, HM, Morrow, DM, Rao, P, Kallal, LA, Moore, ML, Rivero, RA, Palovich, M, Salmon, M, Belmonte, KE & Busch-Petersen, J 2008, 'Discovery of novel and long acting muscarinic acetylcholine receptor antagonists', Journal of Medicinal Chemistry, vol. 51, no. 16, pp. 4866-4869. https://doi.org/10.1021/jm800634k

TY - JOUR

T1 - Discovery of novel and long acting muscarinic acetylcholine receptor antagonists

AU - Jin, Jian

AU - Wang, Yonghui

AU - Shi, Dongchuan

AU - Wang, Feng

AU - Davis, Roderick S.

AU - Jin, Qi

AU - Fu, Wei

AU - Foley, James J.

AU - Webb, Edward F.

AU - Dehaas, Chris J.

AU - Berlanga, Manuela

AU - Burman, Miriam

AU - Sarau, Henry M.

AU - Morrow, Dwight M.

AU - Rao, Parvathi

AU - Kallal, Lorena A.

AU - Moore, Michael L.

AU - Rivero, Ralph A.

AU - Palovich, Michael

AU - Salmon, Michael

AU - Belmonte, Kristen E.

AU - Busch-Petersen, Jakob

PY - 2008/8/28

Y1 - 2008/8/28

N2 - High throughput screening and subsequent optimization led to the discovery of novel quaternary ammonium salts as highly potent muscarinic acetylcholine receptor antagonists with excellent selectivity. Compounds 8a, 13a, and 13b showed excellent inhibitory activity and long duration of action in bronchoconstriction in vivo models in two species via intranasal or intratracheal administration. The novel inhaled muscarinic receptor antagonists are potentially useful therapeutic agents for the treatment of chronic obstructive pulmonary disease and other bronchoconstriction disorders.

AB - High throughput screening and subsequent optimization led to the discovery of novel quaternary ammonium salts as highly potent muscarinic acetylcholine receptor antagonists with excellent selectivity. Compounds 8a, 13a, and 13b showed excellent inhibitory activity and long duration of action in bronchoconstriction in vivo models in two species via intranasal or intratracheal administration. The novel inhaled muscarinic receptor antagonists are potentially useful therapeutic agents for the treatment of chronic obstructive pulmonary disease and other bronchoconstriction disorders.

UR - http://www.scopus.com/inward/record.url?scp=50249177032&partnerID=8YFLogxK

U2 - 10.1021/jm800634k

DO - 10.1021/jm800634k

M3 - Article

C2 - 18680280

AN - SCOPUS:50249177032

SN - 0022-2623

VL - 51

SP - 4866

EP - 4869

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 16

ER -

Discovery of novel and long acting muscarinic acetylcholine receptor antagonists

Abstract

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