2,4-Dicarboxy-pyrroles as Selective Non-Competitive mGluR1 Antagonists: Further Characterization of 3,5-Dimethyl Pyrrole-2,4-dicarboxylic Acid 2-Propyl Ester 4-(1,2,2-Trimethyl-propyl) Ester and Structure—Activity Relationships.

ChemInform ◽  
2003 ◽  
Vol 34 (42) ◽  
Author(s):  
Fabrizio Micheli ◽  
Romano Di Fabio ◽  
et al. et al.
Keyword(s):  
Dicarboxylic Acid ◽  
Structure Activity Relationships ◽  
Propyl Ester ◽  
Structure Activity

scholarly journals Characterization of platinum(II) complexes exhibiting inhibitory activity against the 20S proteasome

2020 ◽  
Vol 7 (8) ◽  
pp. 200545
Author(s):  
Tatsuto Kiwada ◽  
Hiromu Katakasu ◽  
Serina Okumura ◽  
Akira Odani
Keyword(s):  
Inhibitory Activity ◽  
Chemical Structure ◽  
Competitive Inhibition ◽  
Proteasome Inhibitors ◽  
Platinum Complex ◽  
Platinum Complexes ◽  
Binding Mode ◽  
Structure Activity Relationships ◽  
Structure Activity

Proteasome inhibitors are useful for biochemical research and clinical treatment. In our previous study, we reported that the 4N-coordinated platinum complexes with anthracenyl ring and heterocycle exhibited proteasome-inhibitory activity. In the present study, the structure–activity relationships and characterization of these complexes were determined for the elucidation of the role of aromatic ligands. Lineweaver–Burk analysis revealed that the chemical structure of heterocycles affects the binding mode of platinum complexes. Platinum complexes with anthracenyl ring and pyridine showed competitive inhibition, although platinum complexes with anthracenyl ring and phenanthroline showed non-competitive inhibition. The structure–activity relationships demonstrated that anthracenyl moiety plays a crucial role in proteasome-inhibitory activity. The platinum complexes with naphthyl or phenyl rings exhibited lower inhibitory activities than the platinum complex with anthracenyl ring. The reactivity with N-acetylcysteine varied according to the chemical structure of complexes.

Benzophenone dicarboxylic acid antagonists of leukotriene B4. 1. Structure-activity relationships of the benzophenone nucleus

1990 ◽  
Vol 33 (10) ◽  
pp. 2798-2807 ◽  
Author(s):  
D. Mark Gapinski ◽  
Barbara E. Mallett ◽  
Larry L. Froelich ◽  
William T. Jackson
Keyword(s):  
Dicarboxylic Acid ◽  
Leukotriene B4 ◽  
Structure Activity Relationships ◽  
Structure Activity

scholarly journals Identification of the first surrogate agonists for the G protein-coupled receptor GPR132

RSC Advances ◽  
2015 ◽  
Vol 5 (60) ◽  
pp. 48551-48557 ◽  
Author(s):  
Mohamed A. Shehata ◽  
Hanna Belcik Christensen ◽  
Vignir Isberg ◽  
Daniel Sejer Pedersen ◽  
Andreas Bender ◽  
...  
Keyword(s):  
G Protein ◽  
Binding Mode ◽  
Orphan Receptor ◽  
G Protein Coupled Receptor ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
G Protein Coupled

We report the first pharmacological tool agonist for in vitro characterization of the orphan receptor GPR132, preliminary structure–activity relationships based on 32 analogs and a suggested binding mode from docking.

Structure–Activity Relationships and Biological Characterization of a Novel, Potent, and Serum Stable C-X-C Chemokine Receptor Type 4 (CXCR4) Antagonist

2017 ◽  
Vol 60 (23) ◽  
pp. 9641-9652 ◽  
Author(s):  
Salvatore Di Maro ◽  
Francesco Saverio Di Leva ◽  
Anna Maria Trotta ◽  
Diego Brancaccio ◽  
Luigi Portella ◽  
...  
Keyword(s):  
Chemokine Receptor ◽  
Receptor Type ◽  
Biological Characterization ◽  
Cxcr4 Antagonist ◽  
Structure Activity Relationships ◽  
Structure Activity
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