Structure-activity relationship studies of SEN12333 analogues: Determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs

Corinne Beinat; Tristan Reekie; Samuel D. Banister; James O'Brien-Brown; Teresa Xie; Thao T. Olson; Yingxian Xiao; Andrew Harvey; Susan O'Connor; Carolyn Coles; Anton Grishin; Peter Kolesik; John Tsanaktsidis; Michael Kassiou

doi:10.1016/j.ejmech.2015.03.025

Structure-activity relationship studies of SEN12333 analogues: Determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs

Corinne Beinat, Tristan Reekie, Samuel D. Banister, James O'Brien-Brown, Teresa Xie, Thao T. Olson, Yingxian Xiao, Andrew Harvey, Susan O'Connor, Carolyn Coles, Anton Grishin, Peter Kolesik, John Tsanaktsidis, Michael Kassiou^*

^*Corresponding author for this work

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

14 Citations (Scopus)

Abstract

Alpha7 nicotinic acetylcholine receptors (nAChRs) have implications in the regulation of cognitive processes such as memory and attention and have been identified as a promising therapeutic target for the treatment of the cognitive deficits associated with schizophrenia and Alzheimer's disease (AD). Structure affinity relationship studies of the previously described α7 agonist SEN12333 (8), have resulted in the identification of compound 45, a potent and selective agonist of the α7 nAChR with enhanced affinity and improved physicochemical properties over the parent compound (SEN12333, 8).

Original language	English
Pages (from-to)	277-301
Number of pages	25
Journal	European Journal of Medicinal Chemistry
Volume	95
DOIs	https://doi.org/10.1016/j.ejmech.2015.03.025
Publication status	Published - 5 May 2015
Externally published	Yes

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Beinat, C., Reekie, T., Banister, S. D., O'Brien-Brown, J., Xie, T., Olson, T. T., Xiao, Y., Harvey, A., O'Connor, S., Coles, C., Grishin, A., Kolesik, P., Tsanaktsidis, J., & Kassiou, M. (2015). Structure-activity relationship studies of SEN12333 analogues: Determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs. European Journal of Medicinal Chemistry, 95, 277-301. https://doi.org/10.1016/j.ejmech.2015.03.025

@article{bf6825e855994e228a33d1da5cc39f00,

title = "Structure-activity relationship studies of SEN12333 analogues: Determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs",

abstract = "Alpha7 nicotinic acetylcholine receptors (nAChRs) have implications in the regulation of cognitive processes such as memory and attention and have been identified as a promising therapeutic target for the treatment of the cognitive deficits associated with schizophrenia and Alzheimer's disease (AD). Structure affinity relationship studies of the previously described α7 agonist SEN12333 (8), have resulted in the identification of compound 45, a potent and selective agonist of the α7 nAChR with enhanced affinity and improved physicochemical properties over the parent compound (SEN12333, 8).",

keywords = "Acetylcholine receptor, CNS, Structure activity relationships, α7 nicotinic receptors",

author = "Corinne Beinat and Tristan Reekie and Banister, {Samuel D.} and James O'Brien-Brown and Teresa Xie and Olson, {Thao T.} and Yingxian Xiao and Andrew Harvey and Susan O'Connor and Carolyn Coles and Anton Grishin and Peter Kolesik and John Tsanaktsidis and Michael Kassiou",

note = "Publisher Copyright: {\textcopyright} 2015 Elsevier Masson SAS.",

year = "2015",

month = may,

day = "5",

doi = "10.1016/j.ejmech.2015.03.025",

language = "English",

volume = "95",

pages = "277--301",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson s.r.l.",

}

Beinat, C, Reekie, T, Banister, SD, O'Brien-Brown, J, Xie, T, Olson, TT, Xiao, Y, Harvey, A, O'Connor, S, Coles, C, Grishin, A, Kolesik, P, Tsanaktsidis, J & Kassiou, M 2015, 'Structure-activity relationship studies of SEN12333 analogues: Determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs', European Journal of Medicinal Chemistry, vol. 95, pp. 277-301. https://doi.org/10.1016/j.ejmech.2015.03.025

Structure-activity relationship studies of SEN12333 analogues: Determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs. / Beinat, Corinne; Reekie, Tristan; Banister, Samuel D. et al.
In: European Journal of Medicinal Chemistry, Vol. 95, 05.05.2015, p. 277-301.

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

TY - JOUR

T1 - Structure-activity relationship studies of SEN12333 analogues

T2 - Determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs

AU - Beinat, Corinne

AU - Reekie, Tristan

AU - Banister, Samuel D.

AU - O'Brien-Brown, James

AU - Xie, Teresa

AU - Olson, Thao T.

AU - Xiao, Yingxian

AU - Harvey, Andrew

AU - O'Connor, Susan

AU - Coles, Carolyn

AU - Grishin, Anton

AU - Kolesik, Peter

AU - Tsanaktsidis, John

AU - Kassiou, Michael

PY - 2015/5/5

Y1 - 2015/5/5

N2 - Alpha7 nicotinic acetylcholine receptors (nAChRs) have implications in the regulation of cognitive processes such as memory and attention and have been identified as a promising therapeutic target for the treatment of the cognitive deficits associated with schizophrenia and Alzheimer's disease (AD). Structure affinity relationship studies of the previously described α7 agonist SEN12333 (8), have resulted in the identification of compound 45, a potent and selective agonist of the α7 nAChR with enhanced affinity and improved physicochemical properties over the parent compound (SEN12333, 8).

AB - Alpha7 nicotinic acetylcholine receptors (nAChRs) have implications in the regulation of cognitive processes such as memory and attention and have been identified as a promising therapeutic target for the treatment of the cognitive deficits associated with schizophrenia and Alzheimer's disease (AD). Structure affinity relationship studies of the previously described α7 agonist SEN12333 (8), have resulted in the identification of compound 45, a potent and selective agonist of the α7 nAChR with enhanced affinity and improved physicochemical properties over the parent compound (SEN12333, 8).

KW - Acetylcholine receptor

KW - CNS

KW - Structure activity relationships

KW - α7 nicotinic receptors

UR - http://www.scopus.com/inward/record.url?scp=84925448189&partnerID=8YFLogxK

U2 - 10.1016/j.ejmech.2015.03.025

DO - 10.1016/j.ejmech.2015.03.025

M3 - Article

SN - 0223-5234

VL - 95

SP - 277

EP - 301

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

Structure-activity relationship studies of SEN12333 analogues: Determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs

Abstract

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