Bioorganic and Medicinal Chemistry Letters, volume 21, issue 3, pages 940-943

Synthesis and structure–analgesic activity relationships of a novel series of monospirocyclopiperazinium salts (MSPZ)

Publication typeJournal Article
Publication date2011-02-01
Quartile SCImago
Q2
Quartile WOS
Q2
Impact factor2.7
ISSN0960894X, 14643405
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
A series of monospirocyclopiperazinium salts were designed and synthesized to search for a peripherally-acting analgesic drug with low side effects. Extensive SAR studies revealed that a suitable NR(2)R(3) was critical for the analgesic activity, which might be beneficial to expose the cationic nitrogen to bind to the receptor, and possibly interact with the receptor via π-π interaction. Introduction of substituting group on the N(4)-phenyl ring could improve the activity, and the best position was the 4-position. Compound 14n showed more potent analgesic activity (63%, 20 μM/kg, sc) and holds promise for development as a mechanically new analgesic drug.

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GOST Copy
Lin S. W. et al. Synthesis and structure–analgesic activity relationships of a novel series of monospirocyclopiperazinium salts (MSPZ) // Bioorganic and Medicinal Chemistry Letters. 2011. Vol. 21. No. 3. pp. 940-943.
GOST all authors (up to 50) Copy
Lin S. W., Sun Q., Ge Z., Wang X., Ye J., Li R. Synthesis and structure–analgesic activity relationships of a novel series of monospirocyclopiperazinium salts (MSPZ) // Bioorganic and Medicinal Chemistry Letters. 2011. Vol. 21. No. 3. pp. 940-943.
RIS |
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RIS Copy
TY - JOUR
DO - 10.1016/j.bmcl.2010.12.052
UR - https://doi.org/10.1016%2Fj.bmcl.2010.12.052
TI - Synthesis and structure–analgesic activity relationships of a novel series of monospirocyclopiperazinium salts (MSPZ)
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Lin, Song Wen
AU - Sun, Qi
AU - Ge, Ze-mei
AU - Wang, Xin
AU - Ye, Jia
AU - Li, Runtao
PY - 2011
DA - 2011/02/01 00:00:00
PB - Elsevier
SP - 940-943
IS - 3
VL - 21
SN - 0960-894X
SN - 1464-3405
ER -
BibTex |
Cite this
BibTex Copy
@article{2011_Lin
author = {Song Wen Lin and Qi Sun and Ze-mei Ge and Xin Wang and Jia Ye and Runtao Li},
title = {Synthesis and structure–analgesic activity relationships of a novel series of monospirocyclopiperazinium salts (MSPZ)},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2011},
volume = {21},
publisher = {Elsevier},
month = {feb},
url = {https://doi.org/10.1016%2Fj.bmcl.2010.12.052},
number = {3},
pages = {940--943},
doi = {10.1016/j.bmcl.2010.12.052}
}
MLA
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MLA Copy
Lin, Song Wen, et al. “Synthesis and structure–analgesic activity relationships of a novel series of monospirocyclopiperazinium salts (MSPZ).” Bioorganic and Medicinal Chemistry Letters, vol. 21, no. 3, Feb. 2011, pp. 940-943. https://doi.org/10.1016%2Fj.bmcl.2010.12.052.
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