Structure-activity relationships of strychnine analogues at glycine receptors

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

Structure-activity relationships of strychnine analogues at glycine receptors. / Mohsen, A.M.Y.; Heller, Eberhard; Holzgrabe, Ulrike; Jensen, Anders A.; Zlotos, Darius P.

In: Chemistry & Biodiversity, Vol. 11, No. 8, 2014, p. 1256-1262.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Mohsen, AMY, Heller, E, Holzgrabe, U, Jensen, AA & Zlotos, DP 2014, 'Structure-activity relationships of strychnine analogues at glycine receptors', Chemistry & Biodiversity, vol. 11, no. 8, pp. 1256-1262. https://doi.org/10.1002/cbdv.201400110

APA

Mohsen, A. M. Y., Heller, E., Holzgrabe, U., Jensen, A. A., & Zlotos, D. P. (2014). Structure-activity relationships of strychnine analogues at glycine receptors. Chemistry & Biodiversity, 11(8), 1256-1262. https://doi.org/10.1002/cbdv.201400110

Vancouver

Mohsen AMY, Heller E, Holzgrabe U, Jensen AA, Zlotos DP. Structure-activity relationships of strychnine analogues at glycine receptors. Chemistry & Biodiversity. 2014;11(8):1256-1262. https://doi.org/10.1002/cbdv.201400110

Author

Mohsen, A.M.Y. ; Heller, Eberhard ; Holzgrabe, Ulrike ; Jensen, Anders A. ; Zlotos, Darius P. / Structure-activity relationships of strychnine analogues at glycine receptors. In: Chemistry & Biodiversity. 2014 ; Vol. 11, No. 8. pp. 1256-1262.

Bibtex

@article{feda8bfc33814f608f4a3317d574fab0,
title = "Structure-activity relationships of strychnine analogues at glycine receptors",
abstract = "Nine strychnine derivatives including neostrychnine, strychnidine, isostrychnine, 21,22-dihydro-21-hydroxy-22-oxo-strychnine, and several hydrogenated analogs were synthesized, and their antagonistic activities at human α1 and α1β glycine receptors were evaluated. Isostrychnine has shown the best pharmacological profile exhibiting an IC50 value of 1.6 μM at α1 glycine receptors and 3.7-fold preference towards the α1 subtype. SAR Analysis indicates that the lactam moiety and the C(21)[DOUBLE BOND]C(22) bond in strychnine are essential structural features for its high antagonistic potency at glycine receptors",
author = "A.M.Y. Mohsen and Eberhard Heller and Ulrike Holzgrabe and Jensen, {Anders A.} and Zlotos, {Darius P.}",
year = "2014",
doi = "10.1002/cbdv.201400110",
language = "English",
volume = "11",
pages = "1256--1262",
journal = "Chemistry and Biodiversity",
issn = "1612-1872",
publisher = "Wiley - V C H Verlag GmbH & Co. KGaA",
number = "8",

}

RIS

TY - JOUR

T1 - Structure-activity relationships of strychnine analogues at glycine receptors

AU - Mohsen, A.M.Y.

AU - Heller, Eberhard

AU - Holzgrabe, Ulrike

AU - Jensen, Anders A.

AU - Zlotos, Darius P.

PY - 2014

Y1 - 2014

N2 - Nine strychnine derivatives including neostrychnine, strychnidine, isostrychnine, 21,22-dihydro-21-hydroxy-22-oxo-strychnine, and several hydrogenated analogs were synthesized, and their antagonistic activities at human α1 and α1β glycine receptors were evaluated. Isostrychnine has shown the best pharmacological profile exhibiting an IC50 value of 1.6 μM at α1 glycine receptors and 3.7-fold preference towards the α1 subtype. SAR Analysis indicates that the lactam moiety and the C(21)[DOUBLE BOND]C(22) bond in strychnine are essential structural features for its high antagonistic potency at glycine receptors

AB - Nine strychnine derivatives including neostrychnine, strychnidine, isostrychnine, 21,22-dihydro-21-hydroxy-22-oxo-strychnine, and several hydrogenated analogs were synthesized, and their antagonistic activities at human α1 and α1β glycine receptors were evaluated. Isostrychnine has shown the best pharmacological profile exhibiting an IC50 value of 1.6 μM at α1 glycine receptors and 3.7-fold preference towards the α1 subtype. SAR Analysis indicates that the lactam moiety and the C(21)[DOUBLE BOND]C(22) bond in strychnine are essential structural features for its high antagonistic potency at glycine receptors

U2 - 10.1002/cbdv.201400110

DO - 10.1002/cbdv.201400110

M3 - Journal article

C2 - 25146769

VL - 11

SP - 1256

EP - 1262

JO - Chemistry and Biodiversity

JF - Chemistry and Biodiversity

SN - 1612-1872

IS - 8

ER -

ID: 110260067