Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential

Andrew P. Degnan; Darrell Maxwell; Anand Balakrishnan; Jeffrey M. Brown; Amy Easton; Michael Gulianello; Umesh Hanumegowda; Melissa Hill-Drzewi; Regina Miller; Kenneth S. Santone; Arun Senapati; Eric E. Shields; Digavalli V. Sivarao; Ryan Westphal; Valerie J. Whiterock; Xiaoliang Zhuo; Joanne J. Bronson; John E. Macor

doi:10.1016/j.bmcl.2016.11.014

Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential

Andrew P. Degnan
, Darrell Maxwell
, Anand Balakrishnan
, Jeffrey M. Brown
, Amy Easton
, Michael Gulianello
, Umesh Hanumegowda
, Melissa Hill-Drzewi
, Regina Miller
, Kenneth S. Santone
, Arun Senapati
, Eric E. Shields
, Digavalli V. Sivarao
, Ryan Westphal
, Valerie J. Whiterock
, Xiaoliang Zhuo
, Joanne J. Bronson
, John E. Macor

Department of Pharmaceutical Sciences

Bristol-Myers Squibb

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

Original language	English
Pages (from-to)	5871-5876
Number of pages	6
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	26
Issue number	24
DOIs	https://doi.org/10.1016/j.bmcl.2016.11.014
State	Published - 2016

ASJC Scopus Subject Areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Keywords

Bioactivation
Cognition
mGluR5
PAMs
Schizophrenia

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10.1016/j.bmcl.2016.11.014

Cite this

Degnan, A. P., Maxwell, D., Balakrishnan, A., Brown, J. M., Easton, A., Gulianello, M., Hanumegowda, U., Hill-Drzewi, M., Miller, R., Santone, K. S., Senapati, A., Shields, E. E., Sivarao, D. V., Westphal, R., Whiterock, V. J., Zhuo, X., Bronson, J. J., & Macor, J. E. (2016). Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential. Bioorganic and Medicinal Chemistry Letters, 26(24), 5871-5876. https://doi.org/10.1016/j.bmcl.2016.11.014

Degnan, AP, Maxwell, D, Balakrishnan, A, Brown, JM, Easton, A, Gulianello, M, Hanumegowda, U, Hill-Drzewi, M, Miller, R, Santone, KS, Senapati, A, Shields, EE, Sivarao, DV, Westphal, R, Whiterock, VJ, Zhuo, X, Bronson, JJ & Macor, JE 2016, 'Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential', Bioorganic and Medicinal Chemistry Letters, vol. 26, no. 24, pp. 5871-5876. https://doi.org/10.1016/j.bmcl.2016.11.014

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title = "Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential",

keywords = "Bioactivation, Cognition, mGluR5, PAMs, Schizophrenia",

author = "Degnan, \{Andrew P.\} and Darrell Maxwell and Anand Balakrishnan and Brown, \{Jeffrey M.\} and Amy Easton and Michael Gulianello and Umesh Hanumegowda and Melissa Hill-Drzewi and Regina Miller and Santone, \{Kenneth S.\} and Arun Senapati and Shields, \{Eric E.\} and Sivarao, \{Digavalli V.\} and Ryan Westphal and Whiterock, \{Valerie J.\} and Xiaoliang Zhuo and Bronson, \{Joanne J.\} and Macor, \{John E.\}",

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year = "2016",

doi = "10.1016/j.bmcl.2016.11.014",

language = "English",

volume = "26",

pages = "5871--5876",

journal = "Bioorganic and Medicinal Chemistry Letters",

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T1 - Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential

AU - Degnan, Andrew P.

AU - Maxwell, Darrell

AU - Balakrishnan, Anand

AU - Brown, Jeffrey M.

AU - Easton, Amy

AU - Gulianello, Michael

AU - Hanumegowda, Umesh

AU - Hill-Drzewi, Melissa

AU - Miller, Regina

AU - Santone, Kenneth S.

AU - Senapati, Arun

AU - Shields, Eric E.

AU - Sivarao, Digavalli V.

AU - Westphal, Ryan

AU - Whiterock, Valerie J.

AU - Zhuo, Xiaoliang

AU - Bronson, Joanne J.

AU - Macor, John E.

PY - 2016

Y1 - 2016

KW - Bioactivation

KW - Cognition

KW - mGluR5

KW - PAMs

KW - Schizophrenia

UR - https://www.scopus.com/pages/publications/84998610821

UR - https://www.scopus.com/pages/publications/84998610821#tab=citedBy

U2 - 10.1016/j.bmcl.2016.11.014

DO - 10.1016/j.bmcl.2016.11.014

M3 - Article

C2 - 27856084

AN - SCOPUS:84998610821

SN - 0960-894X

VL - 26

SP - 5871

EP - 5876

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 24

ER -

Difluorocyclobutylacetylenes as positive allosteric modulators of mGluR5 with reduced bioactivation potential

ASJC Scopus Subject Areas

Keywords

Access to Document

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