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 type: Journal Article
Publication date: 2011-02-01
Quartile SCImago
Q2
Quartile WOS
Q2
Impact factor: 2.7
ISSN: 0960894X, 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.
Citations by journals
1
|
|
Chemistry of Heterocyclic Compounds
|
Chemistry of Heterocyclic Compounds
1 publication, 7.14%
|
Medicinal Chemistry Research
|
Medicinal Chemistry Research
1 publication, 7.14%
|
Research on Chemical Intermediates
|
Research on Chemical Intermediates
1 publication, 7.14%
|
European Journal of Pharmaceutical Sciences
|
European Journal of Pharmaceutical Sciences
1 publication, 7.14%
|
Polymer
|
Polymer
1 publication, 7.14%
|
Dyes and Pigments
|
Dyes and Pigments
1 publication, 7.14%
|
European Journal of Medicinal Chemistry
|
European Journal of Medicinal Chemistry
1 publication, 7.14%
|
Organic Process Research and Development
|
Organic Process Research and Development
1 publication, 7.14%
|
Journal of Organic Chemistry
|
Journal of Organic Chemistry
1 publication, 7.14%
|
Journal of Agricultural and Food Chemistry
|
Journal of Agricultural and Food Chemistry
1 publication, 7.14%
|
Nanoscale
|
Nanoscale
1 publication, 7.14%
|
Organic Chemistry Frontiers
|
Organic Chemistry Frontiers
1 publication, 7.14%
|
Synthesis
|
Synthesis
1 publication, 7.14%
|
1
|
Citations by publishers
1
2
3
4
|
|
Elsevier
|
Elsevier
4 publications, 28.57%
|
Springer Nature
|
Springer Nature
3 publications, 21.43%
|
American Chemical Society (ACS)
|
American Chemical Society (ACS)
3 publications, 21.43%
|
Royal Society of Chemistry (RSC)
|
Royal Society of Chemistry (RSC)
2 publications, 14.29%
|
Thieme
|
Thieme
1 publication, 7.14%
|
1
2
3
4
|
- We do not take into account publications that without a DOI.
- Statistics recalculated only for publications connected to researchers, organizations and labs registered on the platform.
- Statistics recalculated weekly.
{"yearsCitations":{"type":"bar","data":{"show":true,"labels":[2011,2012,2013,2014,2015,2016,2017,2018,2019,2020,2021,2022,2023],"ids":[0,0,0,0,0,0,0,0,0,0,0,0,0],"codes":[0,0,0,0,0,0,0,0,0,0,0,0,0],"imageUrls":["","","","","","","","","","","","",""],"datasets":[{"label":"Citations number","data":[1,2,2,1,1,1,0,1,0,1,1,2,1],"backgroundColor":["#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6"],"percentage":["7.14","14.29","14.29","7.14","7.14","7.14",0,"7.14",0,"7.14","7.14","14.29","7.14"],"barThickness":null}]},"options":{"indexAxis":"x","maintainAspectRatio":true,"scales":{"y":{"ticks":{"precision":0,"autoSkip":false,"font":{"family":"Montserrat"},"color":"#000000"}},"x":{"ticks":{"stepSize":1,"precision":0,"font":{"family":"Montserrat"},"color":"#000000"}}},"plugins":{"legend":{"position":"top","labels":{"font":{"family":"Montserrat"},"color":"#000000"}},"title":{"display":true,"text":"Citations per year","font":{"size":24,"family":"Montserrat","weight":600},"color":"#000000"}}}},"journals":{"type":"bar","data":{"show":true,"labels":["Chemistry of Heterocyclic Compounds","Medicinal Chemistry Research","Research on Chemical Intermediates","European Journal of Pharmaceutical Sciences","Polymer","Dyes and Pigments","European Journal of Medicinal Chemistry","Organic Process Research and Development","Journal of Organic Chemistry","Journal of Agricultural and Food Chemistry","Nanoscale","Organic Chemistry Frontiers","Synthesis"],"ids":[16828,6106,10787,9338,19955,10101,8171,11058,8697,22576,228,3991,10934],"codes":[0,0,0,0,0,0,0,0,0,0,0,0,0],"imageUrls":["\/storage\/images\/resized\/voXLqlsvTwv5p3iMQ8Dhs95nqB4AXOG7Taj7G4ra_medium.webp","\/storage\/images\/resized\/voXLqlsvTwv5p3iMQ8Dhs95nqB4AXOG7Taj7G4ra_medium.webp","\/storage\/images\/resized\/voXLqlsvTwv5p3iMQ8Dhs95nqB4AXOG7Taj7G4ra_medium.webp","\/storage\/images\/resized\/GDnYOu1UpMMfMMRV6Aqle4H0YLLsraeD9IP9qScG_medium.webp","\/storage\/images\/resized\/GDnYOu1UpMMfMMRV6Aqle4H0YLLsraeD9IP9qScG_medium.webp","\/storage\/images\/resized\/GDnYOu1UpMMfMMRV6Aqle4H0YLLsraeD9IP9qScG_medium.webp","\/storage\/images\/resized\/GDnYOu1UpMMfMMRV6Aqle4H0YLLsraeD9IP9qScG_medium.webp","\/storage\/images\/resized\/iLiQsFqFaSEx6chlGQ5fbAwF6VYU3WWa08hkss0g_medium.webp","\/storage\/images\/resized\/iLiQsFqFaSEx6chlGQ5fbAwF6VYU3WWa08hkss0g_medium.webp","\/storage\/images\/resized\/iLiQsFqFaSEx6chlGQ5fbAwF6VYU3WWa08hkss0g_medium.webp","\/storage\/images\/resized\/leiAYcRDGTSl5B1eCnwpSGqmDEUEfDPPoYisFGhT_medium.webp","\/storage\/images\/resized\/leiAYcRDGTSl5B1eCnwpSGqmDEUEfDPPoYisFGhT_medium.webp","\/storage\/images\/resized\/xqixcltwJYe6H8Uco2JbAFfIOzt7UNKH0OcPOPzO_medium.webp"],"datasets":[{"label":"","data":[1,1,1,1,1,1,1,1,1,1,1,1,1],"backgroundColor":["#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6"],"percentage":[7.14,7.14,7.14,7.14,7.14,7.14,7.14,7.14,7.14,7.14,7.14,7.14,7.14],"barThickness":13}]},"options":{"indexAxis":"y","maintainAspectRatio":false,"scales":{"y":{"ticks":{"precision":0,"autoSkip":false,"font":{"family":"Montserrat"},"color":"#000000"}},"x":{"ticks":{"stepSize":null,"precision":0,"font":{"family":"Montserrat"},"color":"#000000"}}},"plugins":{"legend":{"position":"top","labels":{"font":{"family":"Montserrat"},"color":"#000000"}},"title":{"display":true,"text":"Journals","font":{"size":24,"family":"Montserrat","weight":600},"color":"#000000"}}}},"publishers":{"type":"bar","data":{"show":true,"labels":["Elsevier","Springer Nature","American Chemical Society (ACS)","Royal Society of Chemistry (RSC)","Thieme"],"ids":[17,8,40,123,135],"codes":[0,0,0,0,0],"imageUrls":["\/storage\/images\/resized\/GDnYOu1UpMMfMMRV6Aqle4H0YLLsraeD9IP9qScG_medium.webp","\/storage\/images\/resized\/voXLqlsvTwv5p3iMQ8Dhs95nqB4AXOG7Taj7G4ra_medium.webp","\/storage\/images\/resized\/iLiQsFqFaSEx6chlGQ5fbAwF6VYU3WWa08hkss0g_medium.webp","\/storage\/images\/resized\/leiAYcRDGTSl5B1eCnwpSGqmDEUEfDPPoYisFGhT_medium.webp","\/storage\/images\/resized\/xqixcltwJYe6H8Uco2JbAFfIOzt7UNKH0OcPOPzO_medium.webp"],"datasets":[{"label":"","data":[4,3,3,2,1],"backgroundColor":["#3B82F6","#3B82F6","#3B82F6","#3B82F6","#3B82F6"],"percentage":[28.57,21.43,21.43,14.29,7.14],"barThickness":13}]},"options":{"indexAxis":"y","maintainAspectRatio":false,"scales":{"y":{"ticks":{"precision":0,"autoSkip":false,"font":{"family":"Montserrat"},"color":"#000000"}},"x":{"ticks":{"stepSize":null,"precision":0,"font":{"family":"Montserrat"},"color":"#000000"}}},"plugins":{"legend":{"position":"top","labels":{"font":{"family":"Montserrat"},"color":"#000000"}},"title":{"display":true,"text":"Publishers","font":{"size":24,"family":"Montserrat","weight":600},"color":"#000000"}}}}}
Metrics
Cite this
GOST |
RIS |
BibTex |
MLA
Cite this
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.
Cite this
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 -
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}
}
Cite this
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.