2′ Biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR

Brian Budzik; Vincenzo Garzya; Dongchuan Shi; James J. Foley; Ralph A. Rivero; Christopher J. Langmead; Jeannette Watson; Zining Wu; Ian T. Forbes; Jian Jin

doi:10.1016/j.bmcl.2010.04.128

2′ Biaryl amides as novel and subtype selective M₁ agonists. Part I: Identification, synthesis, and initial SAR

Brian Budzik, Vincenzo Garzya, Dongchuan Shi, James J. Foley, Ralph A. Rivero, Christopher J. Langmead, Jeannette Watson, Zining Wu, Ian T. Forbes, Jian Jin

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

16 Scopus citations

Abstract

Biaryl amides were discovered as novel and subtype selective M₁ muscarinic acetylcholine receptor agonists. The identification, synthesis, and initial structure-activity relationships that led to compounds 3j and 4c, possessing good M₁ agonist potency and intrinsic activity, and subtype selectivity for M₁ over M_2-5, are described.

Original language	English
Pages (from-to)	3540-3544
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	12
DOIs	https://doi.org/10.1016/j.bmcl.2010.04.128
State	Published - 2010
Externally published	Yes

Keywords

2′ Biaryl amides
Novel M1 agonists
Subtype selective M1 muscarinic acetylcholine receptor agonist

Access to Document

10.1016/j.bmcl.2010.04.128

Cite this

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title = "2′ Biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR",

abstract = "Biaryl amides were discovered as novel and subtype selective M1 muscarinic acetylcholine receptor agonists. The identification, synthesis, and initial structure-activity relationships that led to compounds 3j and 4c, possessing good M1 agonist potency and intrinsic activity, and subtype selectivity for M1 over M2-5, are described.",

keywords = "2′ Biaryl amides, Novel M1 agonists, Subtype selective M1 muscarinic acetylcholine receptor agonist",

author = "Brian Budzik and Vincenzo Garzya and Dongchuan Shi and Foley, \{James J.\} and Rivero, \{Ralph A.\} and Langmead, \{Christopher J.\} and Jeannette Watson and Zining Wu and Forbes, \{Ian T.\} and Jian Jin",

year = "2010",

doi = "10.1016/j.bmcl.2010.04.128",

language = "English",

volume = "20",

pages = "3540--3544",

journal = "Bioorganic and Medicinal Chemistry Letters",

issn = "0960-894X",

publisher = "Elsevier Ltd.",

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TY - JOUR

T1 - 2′ Biaryl amides as novel and subtype selective M1 agonists. Part I

T2 - Identification, synthesis, and initial SAR

AU - Budzik, Brian

AU - Garzya, Vincenzo

AU - Shi, Dongchuan

AU - Foley, James J.

AU - Rivero, Ralph A.

AU - Langmead, Christopher J.

AU - Watson, Jeannette

AU - Wu, Zining

AU - Forbes, Ian T.

AU - Jin, Jian

PY - 2010

Y1 - 2010

N2 - Biaryl amides were discovered as novel and subtype selective M1 muscarinic acetylcholine receptor agonists. The identification, synthesis, and initial structure-activity relationships that led to compounds 3j and 4c, possessing good M1 agonist potency and intrinsic activity, and subtype selectivity for M1 over M2-5, are described.

AB - Biaryl amides were discovered as novel and subtype selective M1 muscarinic acetylcholine receptor agonists. The identification, synthesis, and initial structure-activity relationships that led to compounds 3j and 4c, possessing good M1 agonist potency and intrinsic activity, and subtype selectivity for M1 over M2-5, are described.

KW - 2′ Biaryl amides

KW - Novel M1 agonists

KW - Subtype selective M1 muscarinic acetylcholine receptor agonist

UR - https://www.scopus.com/pages/publications/77954217196

U2 - 10.1016/j.bmcl.2010.04.128

DO - 10.1016/j.bmcl.2010.04.128

M3 - Article

C2 - 20483611

AN - SCOPUS:77954217196

SN - 0960-894X

VL - 20

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EP - 3544

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 12