2-Phenylpyrroles as conformationally restricted benzamide analogs. A new class of potential antipsychotics. 1

1987 ◽  
Vol 30 (11) ◽  
pp. 2099-2104 ◽  
Author(s):  
Ineke Van Wijngaarden ◽  
Chris G. Kruse ◽  
Roelof Van Hes ◽  
Jan A. M. Van der Heyden ◽  
Martin T. M. Tulp
Keyword(s):  
Conformationally Restricted ◽  
New Class

ChemInform Abstract: 2-Phenylpyrroles as Conformationally Restricted Benzamide Analogues. A New Class of Potential Antipsychotics. Part 1.

ChemInform ◽  
1988 ◽  
Vol 19 (15) ◽  
Author(s):  
I. VAN WIJNGAARDEN ◽  
C. G. KRUSE ◽  
R. VAN HES ◽  
J. A. M. VAN DER HEYDEN ◽  
M. TH. M. TULP
Keyword(s):  
Conformationally Restricted ◽  
New Class

Renin inhibitors. Design and synthesis of a new class of conformationally restricted analogs of angiotensinogen

1988 ◽  
Vol 31 (2) ◽  
pp. 284-295 ◽  
Author(s):  
Hing L. Sham ◽  
Giorgio Bolis ◽  
Herman H. Stein ◽  
Stephen W. Fesik ◽  
Patrick A. Marcotte ◽  
...  
Keyword(s):  
Renin Inhibitors ◽  
Conformationally Restricted ◽  
Design And Synthesis ◽  
New Class ◽  
Conformationally Restricted Analogs

scholarly journals Discovery and synthesis of hydroxy-L-proline based blockers of the neutral amino acid transporters SLC1A4 (ASCT1) and SLC1A5 (ASCT2).

2021 ◽  
Author(s):  
Michael P Kavanaugh ◽  
Brent R. Lyda ◽  
Gregory P. Leary ◽  
Derek Silvius ◽  
Nicholas R. Natale ◽  
...  
Keyword(s):  
Amino Acid ◽  
Homology Model ◽  
Neutral Amino Acid ◽  
Amino Acid Transporters ◽  
Biological Targets ◽  
Conformationally Restricted ◽  
New Class ◽  
Wide Range ◽  
Ligand Binding Sites ◽  
Proline Derivatives

The conformationally restricted heterocycle hydroxy-ʟ-proline is a versatile scaffold for the synthesis of diverse multi-functionalized pyrrolidines for probing the ligand binding sites of biological targets. With the goal to develop new inhibitors of the widely expressed amino acid transporters SLC1A4 and SLC1A5 (also known as ASCT1 and ASCT2), we synthesized and functionally screened a series of hydroxy-ʟ-proline derivatives or 'prolinols' using electrophysiological and radio-labeled uptake assays on amino acid transporters from the SLC1, SLC7, and SLC38 solute carrier families. We identified a number of synthetic prolinols that act as selective high-affinity inhibitors of the SLC1 functional subfamily comprising the neutral amino acid transporters SLC1A4 and SLC1A5. The active and inactive prolinols were computationally docked into a threaded homology model and analyzed with respect to predicted molecular orientation and observed pharmacological activity. The series of hydroxy-L-proline derivatives identified here represents a new class of potential agents to pharmacologically modulate SLC1A4 and SLC1A5, amino acid exchangers that play important roles in a wide range of physiological and pathophysiological processes.

scholarly journals Glutathione peroxidase mimics based on conformationally-restricted, peri-like, 4,5-disubstituted fluorene dichalcogenides

2021 ◽  
Author(s):  
Kesar Jagdev ◽  
Damiano Tanini ◽  
Jack W. Lownes ◽  
Carlotta Figliola ◽  
Louise Male ◽  
...  
Keyword(s):  
Glutathione Peroxidase ◽  
Structure And Properties ◽  
Conformationally Restricted ◽  
New Class ◽  
Peroxidase Mimics ◽  
Glutathione Peroxidase Mimics

The synthesis, structure and properties of 4,5-(bay)-substituted fluorene dichalcogenides and their oxides are investigated towards a new class of GPx mimic.

Conformationally restricted novel pyrazole derivatives: Synthesis of 1,8-disubstituted 5,5-dimethyl-4,5-dihydro-1H-benzo[g]indazoles as a new class of PDE4 inhibitors

2012 ◽  
Vol 22 (9) ◽  
pp. 3248-3255 ◽  
Author(s):  
T. Shyamsunder Reddy ◽  
K. Shiva Kumar ◽  
Chandana L.T. Meda ◽  
Ajit Kandale ◽  
D. Rambabu ◽  
...  
Keyword(s):  
Pyrazole Derivatives ◽  
Conformationally Restricted ◽  
New Class

2-Phenylpyrroles as conformationally restricted benzamide analogs. A new class of potential antipsychotics. 2

1988 ◽  
Vol 31 (10) ◽  
pp. 1934-1940 ◽  
Author(s):  
Ineke Van Wijngaarden ◽  
Chris G. Kruse ◽  
Jan A. M. Van der Heyden ◽  
Martin T. M. Tulp
Keyword(s):  
Conformationally Restricted ◽  
New Class

ChemInform Abstract: 2-Phenylpyrroles as Conformationally Restricted Benzamide Analogues. A New Class of Potential Antipsychotics. Part 2.

ChemInform ◽  
1989 ◽  
Vol 20 (10) ◽  
Author(s):  
I. VAN WIJNGAARDEN ◽  
C. G. KRUSE ◽  
J. A. M. VAN DER HEYDEN ◽  
M. T. M. TULP
Keyword(s):  
Conformationally Restricted ◽  
New Class
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