Synthesis and Benzodiazepine Receptor Affinity of Pyrazolo[1,5-a]pyrimidine Derivatives. 3. New 6-(3-Thienyl) Series as α1 Selective Ligands
Silvia Selleri
1
,
Fabrizio Bruni
1
,
Camilla Costagli
1
,
Annarella Costanzo
1
,
Gabriella Guerrini
1
,
Giovanna Ciciani
1
,
Paola Gratteri
1
,
Claudia Bonaccini
1
,
Petra Malmberg-Aiello
1
,
François Besnard
1
,
Stéphane Renard
1
,
Barbara Costa
1
,
Claudia Martini
1
Publication type: Journal Article
Publication date: 2002-12-11
scimago Q1
wos Q1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
12519068
Drug Discovery
Molecular Medicine
Abstract
New 3-aryl-6-(3-thienyl)pyrazolo[1,5-a]pyrimidin-7-ones (2a-j) are synthesized and evaluated in vitro on Bz/GABA(A) receptors and on recombinant benzodiazepine receptors (alpha x beta 2/3 gamma 2; x = 1-3, 5) expressed in HEK293 cells. SAR studies on the new compounds are conducted and molecular modeling is accomplished to better investigate requirements leading to subtype selectivity. Some of the synthesized compounds are tested in vivo to explore their pharmacological effect as a consequence of their high alpha 1 beta 2 gamma 2 subtype selectivity observed in vitro.
Found
Nothing found, try to update filter.
Found
Nothing found, try to update filter.
Top-30
Journals
|
1
2
3
4
5
|
|
|
Synthetic Communications
5 publications, 13.51%
|
|
|
Bioorganic and Medicinal Chemistry
3 publications, 8.11%
|
|
|
Tetrahedron
3 publications, 8.11%
|
|
|
Chemistry of Heterocyclic Compounds
2 publications, 5.41%
|
|
|
Journal of Combinatorial Chemistry
2 publications, 5.41%
|
|
|
Chemistry and Biodiversity
2 publications, 5.41%
|
|
|
Progress in Heterocyclic Chemistry
2 publications, 5.41%
|
|
|
Pharmacological Reviews
1 publication, 2.7%
|
|
|
Letters in Organic Chemistry
1 publication, 2.7%
|
|
|
Current Organic Synthesis
1 publication, 2.7%
|
|
|
Current Pharmaceutical Design
1 publication, 2.7%
|
|
|
Molecules
1 publication, 2.7%
|
|
|
Bioorganic and Medicinal Chemistry Letters
1 publication, 2.7%
|
|
|
European Journal of Medicinal Chemistry
1 publication, 2.7%
|
|
|
Journal of Fluorine Chemistry
1 publication, 2.7%
|
|
|
ChemistrySelect
1 publication, 2.7%
|
|
|
Journal of Medicinal Chemistry
1 publication, 2.7%
|
|
|
Journal of Organic Chemistry
1 publication, 2.7%
|
|
|
Organic and Biomolecular Chemistry
1 publication, 2.7%
|
|
|
RSC Medicinal Chemistry
1 publication, 2.7%
|
|
|
Heterocycles
1 publication, 2.7%
|
|
|
Mendeleev Communications
1 publication, 2.7%
|
|
|
Journal of Heterocyclic Chemistry
1 publication, 2.7%
|
|
|
Journal of Molecular Structure
1 publication, 2.7%
|
|
|
1
2
3
4
5
|
Publishers
|
2
4
6
8
10
12
|
|
|
Elsevier
12 publications, 32.43%
|
|
|
Taylor & Francis
5 publications, 13.51%
|
|
|
Wiley
4 publications, 10.81%
|
|
|
American Chemical Society (ACS)
4 publications, 10.81%
|
|
|
Bentham Science Publishers Ltd.
3 publications, 8.11%
|
|
|
Springer Nature
2 publications, 5.41%
|
|
|
Royal Society of Chemistry (RSC)
2 publications, 5.41%
|
|
|
American Society for Pharmacology and Experimental Therapeutics
1 publication, 2.7%
|
|
|
MDPI
1 publication, 2.7%
|
|
|
The Japan Institute of Heterocyclic Chemistry
1 publication, 2.7%
|
|
|
OOO Zhurnal "Mendeleevskie Soobshcheniya"
1 publication, 2.7%
|
|
|
2
4
6
8
10
12
|
- We do not take into account publications without a DOI.
- Statistics recalculated weekly.
Are you a researcher?
Create a profile to get free access to personal recommendations for colleagues and new articles.
Metrics
37
Total citations:
37
Citations from 2025:
2
(5.41%)
Cite this
GOST |
RIS |
BibTex |
MLA
Cite this
GOST
Copy
Selleri S. et al. Synthesis and Benzodiazepine Receptor Affinity of Pyrazolo[1,5-a]pyrimidine Derivatives. 3. New 6-(3-Thienyl) Series as α1 Selective Ligands // Journal of Medicinal Chemistry. 2002. Vol. 46. No. 2. pp. 310-313.
GOST all authors (up to 50)
Copy
Selleri S., Bruni F., Costagli C., Costanzo A., Guerrini G., Ciciani G., Gratteri P., Bonaccini C., Malmberg-Aiello P., Besnard F., Renard S., Costa B., Martini C. Synthesis and Benzodiazepine Receptor Affinity of Pyrazolo[1,5-a]pyrimidine Derivatives. 3. New 6-(3-Thienyl) Series as α1 Selective Ligands // Journal of Medicinal Chemistry. 2002. Vol. 46. No. 2. pp. 310-313.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1021/jm020999w
UR - https://doi.org/10.1021/jm020999w
TI - Synthesis and Benzodiazepine Receptor Affinity of Pyrazolo[1,5-a]pyrimidine Derivatives. 3. New 6-(3-Thienyl) Series as α1 Selective Ligands
T2 - Journal of Medicinal Chemistry
AU - Selleri, Silvia
AU - Bruni, Fabrizio
AU - Costagli, Camilla
AU - Costanzo, Annarella
AU - Guerrini, Gabriella
AU - Ciciani, Giovanna
AU - Gratteri, Paola
AU - Bonaccini, Claudia
AU - Malmberg-Aiello, Petra
AU - Besnard, François
AU - Renard, Stéphane
AU - Costa, Barbara
AU - Martini, Claudia
PY - 2002
DA - 2002/12/11
PB - American Chemical Society (ACS)
SP - 310-313
IS - 2
VL - 46
PMID - 12519068
SN - 0022-2623
SN - 1520-4804
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2002_Selleri,
author = {Silvia Selleri and Fabrizio Bruni and Camilla Costagli and Annarella Costanzo and Gabriella Guerrini and Giovanna Ciciani and Paola Gratteri and Claudia Bonaccini and Petra Malmberg-Aiello and François Besnard and Stéphane Renard and Barbara Costa and Claudia Martini},
title = {Synthesis and Benzodiazepine Receptor Affinity of Pyrazolo[1,5-a]pyrimidine Derivatives. 3. New 6-(3-Thienyl) Series as α1 Selective Ligands},
journal = {Journal of Medicinal Chemistry},
year = {2002},
volume = {46},
publisher = {American Chemical Society (ACS)},
month = {dec},
url = {https://doi.org/10.1021/jm020999w},
number = {2},
pages = {310--313},
doi = {10.1021/jm020999w}
}
Cite this
MLA
Copy
Selleri, Silvia, et al. “Synthesis and Benzodiazepine Receptor Affinity of Pyrazolo[1,5-a]pyrimidine Derivatives. 3. New 6-(3-Thienyl) Series as α1 Selective Ligands.” Journal of Medicinal Chemistry, vol. 46, no. 2, Dec. 2002, pp. 310-313. https://doi.org/10.1021/jm020999w.