Design, Synthesis, and SAR of Tachykinin Antagonists:  Modulation of Balance in NK1/NK2Receptor Antagonist Activity

2002 ◽  
Vol 45 (18) ◽  
pp. 3972-3983 ◽  
Author(s):  
Jeffrey S. Albert ◽  
David Aharony ◽  
Donald Andisik ◽  
Herbert Barthlow ◽  
Peter R. Bernstein ◽  
...  
Keyword(s):  
Antagonist Activity ◽  
Design Synthesis ◽  
Tachykinin Antagonists

Design, Synthesis, and Calcium Channel Antagonist Activity of New 1,4-Dihydropyridines Containing 4-(5)-Chloro-2-ethyl-5-(4)-imidazolyl Substituent

2006 ◽  
Vol 339 (6) ◽  
pp. 299-304 ◽  
Author(s):  
Asghar Davood ◽  
Niloufar Mansouri ◽  
Ahmad Rerza Dehpour ◽  
Hamed Shafaroudi ◽  
Eskandar Alipour ◽  
...  
Keyword(s):  
Calcium Channel ◽  
Calcium Channel Antagonist ◽  
Antagonist Activity ◽  
Design Synthesis

Design, synthesis, and in vitro activity of bis(succinimido)hexane peptide heterodimers with combined B1 and B2 antagonist activity

1994 ◽  
Vol 37 (3) ◽  
pp. 348-355 ◽  
Author(s):  
John C. Cheronis ◽  
Eric T. Whalley ◽  
Lisa G. Allen ◽  
Sharon D. Loy ◽  
Megan W. Elder ◽  
...  
Keyword(s):  
Vitro Activity ◽  
In Vitro Activity ◽  
Antagonist Activity ◽  
Design Synthesis

Design, Synthesis, and Calcium Channel Antagonist Activity of New 1,4-Dihydropyridines Containing 4-(5)-Chloro-2-ethyl-5-(4)-imidazolyl Substituent.

ChemInform ◽  
2006 ◽  
Vol 37 (39) ◽  
Author(s):  
Asghar Davood ◽  
Niloufar Mansouri ◽  
Ahmad Rerza Dehpour ◽  
Hamed Shafaroudi ◽  
Eskandar Alipour ◽  
...  
Keyword(s):  
Calcium Channel ◽  
Calcium Channel Antagonist ◽  
Antagonist Activity ◽  
Design Synthesis

Design, synthesis, and biological evaluation of new raloxifene analogues of improved antagonist activity and endometrial safety

2021 ◽  
Vol 106 ◽  
pp. 104482
Author(s):  
George Lambrinidis ◽  
Cedric Gouedard ◽  
Sotiria Stasinopoulou ◽  
Angeliki Angelopoulou ◽  
Vassiliki Ganou ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Antagonist Activity ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

Self-Assembly of Hydrogels From Elastin-Mimetic Block Copolymers

2002 ◽  
Vol 724 ◽  
Author(s):  
Elizabeth R. Wright ◽  
R. Andrew McMillan ◽  
Alan Cooper ◽  
Robert P. Apkarian ◽  
Vincent P. Conticello
Keyword(s):  
Block Copolymers ◽  
Self Assembly ◽  
Triblock Copolymers ◽  
Variable Temperature ◽  
Inverse Temperature ◽  
Temperature Transition ◽  
Scanning Calorimetry ◽  
Design Synthesis ◽  
Inverse Temperature Transition ◽  
Functional Biomaterials

AbstractTriblock copolymers have traditionally been synthesized with conventional organic components. However, triblock copolymers could be synthesized by the incorporation of two incompatible protein-based polymers. The polypeptides would differ in their hydrophobicity and confer unique physiochemical properties to the resultant materials. One protein-based polymer, based on a sequence of native elastin, that has been utilized in the synthesis of biomaterials is poly (Valine-Proline-Glycine-ValineGlycine) or poly(VPGVG) [1]. This polypeptide has been shown to have an inverse temperature transition that can be adjusted by non-conservative amino acid substitutions in the fourth position [2]. By combining polypeptide blocks with different inverse temperature transition values due to hydrophobicity differences, we expect to produce amphiphilic polypeptides capable of self-assembly into hydrogels. Our research examines the design, synthesis and characterization of elastin-mimetic block copolymers as functional biomaterials. The methods that are used for the characterization include variable temperature 1D and 2D High-Resolution-NMR, cryo-High Resolutions Scanning Electron Microscopy and Differential Scanning Calorimetry.

Discovery of Antibacterial Agents Inhibiting the Energy-Coupling Factor (ECF) Transporters by Structure-Based Virtual Screening

2020 ◽  
Author(s):  
Eleonora Diamanti ◽  
Inda Setyawati ◽  
Spyridon Bousis ◽  
leticia mojas ◽  
lotteke Swier ◽  
...  
Keyword(s):  
Virtual Screening ◽  
Antibacterial Agents ◽  
Antimicrobial Agents ◽  
Energy Coupling ◽  
Coupling Factor ◽  
Design Synthesis ◽  
Screening Design ◽  
Starting Point ◽  
Wide Range ◽  
Vitamin Uptake

Here, we report on the virtual screening, design, synthesis and structure–activity relationships (SARs) of the first class of selective, antibacterial agents against the energy-coupling factor (ECF) transporters. The ECF transporters are a family of transmembrane proteins involved in the uptake of vitamins in a wide range of bacteria. Inhibition of the activity of these proteins could reduce the viability of pathogens that depend on vitamin uptake. Because of their central role in the metabolism of bacteria and their absence in humans, ECF transporters are novel potential antimicrobial targets to tackle infection. The hit compound’s metabolic and plasma stability, the potency (20, MIC Streptococcus pneumoniae = 2 µg/mL), the absence of cytotoxicity and a lack of resistance development under the conditions tested here suggest that this scaffold may represent a promising starting point for the development of novel antimicrobial agents with an unprecedented mechanism of action.<br>

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