Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst3 receptor antagonists
Thomas Troxler
1
,
Konstanze Hurth
1
,
Karl Heinrich Schuh
1
,
Philippe Schoeffter
2
,
Daniel Langenegger
2
,
Albert Enz
2
,
Daniel Hoyer
2
1
Novartis Institutes for BioMedical Research, Global Discovery Chemistry-Neuroscience, CH-4002 Basel, Switzerland.
|
2
Novartis Institutes for BioMedical Research, Neuroscience Disease Area, CH-4002 Basel, Switzerland
|
Publication type: Journal Article
Publication date: 2010-03-01
scimago Q2
wos Q2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
20137944
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
Starting from non-peptidic sst(1)-selective somatostatin receptor antagonists, first compounds with mixed sst(1)/sst(3) affinity were identified by directed structural modifications. Systematic optimization of these initial leads afforded novel, enantiomerically pure, highly potent and sst(3)-subtype selective somatostatin antagonists based on a (4S,4aS,8aR)-decahydroisoquinoline-4-carboxylic acid core moiety. These compounds can efficiently be synthesized and show promising PK properties in rodents.
Found
Nothing found, try to update filter.
Found
Nothing found, try to update filter.
Top-30
Journals
|
1
2
3
|
|
|
ACS Medicinal Chemistry Letters
3 publications, 18.75%
|
|
|
Pharmacological Reviews
1 publication, 6.25%
|
|
|
Molecular Endocrinology
1 publication, 6.25%
|
|
|
Tetrahedron
1 publication, 6.25%
|
|
|
Pharmacology and Therapeutics
1 publication, 6.25%
|
|
|
Journal of Molecular Catalysis B Enzymatic
1 publication, 6.25%
|
|
|
Journal of Organic Chemistry
1 publication, 6.25%
|
|
|
Journal of Medicinal Chemistry
1 publication, 6.25%
|
|
|
Chemical Society Reviews
1 publication, 6.25%
|
|
|
Chemical Communications
1 publication, 6.25%
|
|
|
Topics in Heterocyclic Chemistry
1 publication, 6.25%
|
|
|
Neuroendocrinology
1 publication, 6.25%
|
|
|
Frontiers in Endocrinology
1 publication, 6.25%
|
|
|
1
2
3
|
Publishers
|
1
2
3
4
5
|
|
|
American Chemical Society (ACS)
5 publications, 31.25%
|
|
|
Elsevier
4 publications, 25%
|
|
|
Royal Society of Chemistry (RSC)
2 publications, 12.5%
|
|
|
American Society for Pharmacology and Experimental Therapeutics
1 publication, 6.25%
|
|
|
The Endocrine Society
1 publication, 6.25%
|
|
|
Springer Nature
1 publication, 6.25%
|
|
|
S. Karger AG
1 publication, 6.25%
|
|
|
Frontiers Media S.A.
1 publication, 6.25%
|
|
|
1
2
3
4
5
|
- 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
16
Total citations:
16
Citations from 2024:
1
(6%)
Cite this
GOST |
RIS |
BibTex |
MLA
Cite this
GOST
Copy
Troxler T. et al. Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst3 receptor antagonists // Bioorganic and Medicinal Chemistry Letters. 2010. Vol. 20. No. 5. pp. 1728-1734.
GOST all authors (up to 50)
Copy
Troxler T., Hurth K., Schuh K. H., Schoeffter P., Langenegger D., Enz A., Hoyer D. Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst3 receptor antagonists // Bioorganic and Medicinal Chemistry Letters. 2010. Vol. 20. No. 5. pp. 1728-1734.
Cite this
RIS
Copy
TY - JOUR
DO - 10.1016/j.bmcl.2010.01.063
UR - https://doi.org/10.1016/j.bmcl.2010.01.063
TI - Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst3 receptor antagonists
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Troxler, Thomas
AU - Hurth, Konstanze
AU - Schuh, Karl Heinrich
AU - Schoeffter, Philippe
AU - Langenegger, Daniel
AU - Enz, Albert
AU - Hoyer, Daniel
PY - 2010
DA - 2010/03/01
PB - Elsevier
SP - 1728-1734
IS - 5
VL - 20
PMID - 20137944
SN - 0960-894X
SN - 1464-3405
ER -
Cite this
BibTex (up to 50 authors)
Copy
@article{2010_Troxler,
author = {Thomas Troxler and Konstanze Hurth and Karl Heinrich Schuh and Philippe Schoeffter and Daniel Langenegger and Albert Enz and Daniel Hoyer},
title = {Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst3 receptor antagonists},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2010},
volume = {20},
publisher = {Elsevier},
month = {mar},
url = {https://doi.org/10.1016/j.bmcl.2010.01.063},
number = {5},
pages = {1728--1734},
doi = {10.1016/j.bmcl.2010.01.063}
}
Cite this
MLA
Copy
Troxler, Thomas, et al. “Decahydroisoquinoline derivatives as novel non-peptidic, potent and subtype-selective somatostatin sst3 receptor antagonists.” Bioorganic and Medicinal Chemistry Letters, vol. 20, no. 5, Mar. 2010, pp. 1728-1734. https://doi.org/10.1016/j.bmcl.2010.01.063.