Elucidation of structure-activity relationships of 2-amino-3-benzoylthiophenes: Study of their allosteric enhancing vs. antagonistic activity on adenosine A1 receptors

2000 ◽  
Vol 49 (4) ◽  
pp. 227-237 ◽  
Author(s):  
Angeliki P. Kourounakis ◽  
Pieter A.M. Van der Klein ◽  
Ad P. Ijzerman
Keyword(s):  
Antagonistic Activity ◽  
Adenosine A1 Receptors ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Adenosine A1

Structure-Activity Relationships of Adenosine A1 and A2 Receptors

1990 ◽  
pp. 57-103 ◽  
Author(s):  
Bharat K. Trivedi ◽  
Alexander J. Bridges ◽  
Robert F. Bruns
Keyword(s):  
Structure Activity Relationships ◽  
Structure Activity ◽  
Adenosine A1 ◽  
A2 Receptors

N9-Benzyl-substituted 1,3-dimethyl- and 1,3-dipropyl-pyrimido[2,1-f]purinediones: Synthesis and structure–activity relationships at adenosine A1 and A2A receptors

2007 ◽  
Vol 15 (14) ◽  
pp. 5003-5017 ◽  
Author(s):  
Anna Drabczyńska ◽  
Christa E. Müller ◽  
Janina Karolak-Wojciechowska ◽  
Britta Schumacher ◽  
Anke Schiedel ◽  
...  
Keyword(s):  
Structure Activity Relationships ◽  
A2a Receptors ◽  
Structure Activity ◽  
Adenosine A1

Pharmacology and quantitative structure-activity relationships of imidazolylpropylguanidines with mepyramine-like substructures as non-peptide neuropeptide Y Y1 receptor antagonists

2000 ◽  
Vol 78 (2) ◽  
pp. 108-115 ◽  
Author(s):  
Stefan Dove ◽  
Martin C Michel ◽  
Sebastian Knieps ◽  
Armin Buschauer
Keyword(s):  
Neuropeptide Y ◽  
Amino Nitrogen ◽  
Phenyl Group ◽  
Antagonistic Activity ◽  
Pyridyl Ring ◽  
Moderate Degree ◽  
Quantitative Structure ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Quantitative Structure Activity Relationships

The design of non-peptide, Y1-selective antagonists of neuropeptide Y (NPY) as pharmacological tools is in progress and is increasingly important as therapeutic applications are expected. Starting from the potent histamine H2 agonist and weak NPY Y1 antagonist arpromidine, 16 imidazolylpropylguanidine derivatives were synthesized and tested for Y1 antagonistic activity (inhibition of NPY-stimulated Ca2+ increase in human erythroleukemic cells), where the pheniramine-like moiety of arpromidine was replaced with 2-pyridylaminoalkyl, benzyl-(2-pyridyl)aminoalkyl, and phenyl-(2-pyridyl)alkylaminoalkyl partial structures derived from mepyramine. The pA2 values of the most active compounds are in the range of 6.2-6.5. Quantitative structure-activity relationships (QSAR) were investigated by fragment regression analysis. Results indicate that a tetramethylene spacer between the guanidino group and the amino nitrogen is optimal. For an at least moderate degree of Y1 antagonistic activity, a second benzyl or phenyl group must be present in addition to the 2-pyridyl ring. At this second group, hydrophobic substituents such as 3,4-di-Cl and 4-Br further enhance Y1 antagonism. The most active derivative additionally bears a 5-Br substituent at the 2-pyridyl moiety. Structure-activity relationships suggest that the compounds might be able to partially imitate the role of NPY when interacting with Y1 receptors and thus behave as moderate non-peptide NPY Y1 antagonists.Key words : neuropeptide Y Y1 antagonists, imidazolylpropylguanidines, quantitative structure-activity relationships.

Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure

1992 ◽  
Vol 35 (16) ◽  
pp. 3066-3075 ◽  
Author(s):  
Fumio Suzuki ◽  
Junichi Shimada ◽  
Hideaki Mizumoto ◽  
Akira Karasawa ◽  
Kazuhiro Kubo ◽  
...  
Keyword(s):  
Renal Failure ◽  
Acute Renal Failure ◽  
Protective Effects ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Adenosine A1

N9-Benzyl-Substituted 1,3-Dimethyl- and 1,3-Dipropyl-pyrimido[2,1-f]purinediones (III): Synthesis and Structure—Activity Relationships at Adenosine A1 and A2A Receptors.

ChemInform ◽  
2007 ◽  
Vol 38 (43) ◽  
Author(s):  
Anna Drabczynska ◽  
Christa E. Mueller ◽  
Janina Karolak-Wojciechowska ◽  
Britta Schumacher ◽  
Anke Schiedel ◽  
...  
Keyword(s):  
Structure Activity Relationships ◽  
A2a Receptors ◽  
Structure Activity ◽  
Adenosine A1

Phenylethyl-substituted pyrimido[2,1-f]purinediones and related compounds: Structure–activity relationships as adenosine A1 and A2A receptor ligands

2007 ◽  
Vol 15 (22) ◽  
pp. 6956-6974 ◽  
Author(s):  
Anna Drabczyńska ◽  
Christa E. Müller ◽  
Anke Schiedel ◽  
Britta Schumacher ◽  
Janina Karolak-Wojciechowska ◽  
...  
Keyword(s):  
Receptor Ligands ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
A2a Receptor ◽  
Adenosine A1 ◽  
Related Compounds
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