ChemInform Abstract: 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.

ChemInform ◽  
2012 ◽  
Vol 43 (39) ◽  
pp. no-no
Author(s):  
S. Venkataiah ◽  
et al. et al.
Keyword(s):  
Pyrazole Derivatives ◽  
Conformationally Restricted ◽  
New Class

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

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

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

Synthesis of benzofuran based 1,3,5-substituted pyrazole derivatives: As a new class of potent antioxidants and antimicrobials-A novel accost to amend biocompatibility

2012 ◽  
Vol 22 (14) ◽  
pp. 4773-4777 ◽  
Author(s):  
Javarappa Rangaswamy ◽  
Honnaiah Vijay Kumar ◽  
Salakatte Thammaiah Harini ◽  
Nagaraja Naik
Keyword(s):  
Pyrazole Derivatives ◽  
New Class

Pyrazole and imidazo[1,2-b]pyrazole Derivatives as New Potential Antituberculosis Agents

2019 ◽  
Vol 15 (1) ◽  
pp. 17-27 ◽  
Author(s):  
Elda Meta ◽  
Chiara Brullo ◽  
Michele Tonelli ◽  
Scott G. Franzblau ◽  
Yuehong Wang ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Pyrazole Derivatives ◽  
Antitubercular Agents ◽  
Active Compounds ◽  
Protein Targets ◽  
Preliminary Screening ◽  
New Class ◽  
Structure Activity ◽  
Starting Point

Background: We screened a large library of differently decorated imidazo-pyrazole and pyrazole derivatives as possible new antitubercular agents and this preliminary screening showed that many compounds are able to totally inhibit Mycobacterium growth (>90 %). Among the most active compounds, we selected some new possible hits based on their similarities and, at the same time, on their novelty with respect to the pipeline drugs. </P><P> Methods: In order to increase the potency and obtain more information about structure-activity relationship (SAR), we designed and synthesized three new series of compounds (2a–e, 3a–e, and 4a–l). Conclusion: Performed tests confirmed that both new pyrazoles and imidazo-pyrazoles could represent a new starting point to obtain more potent compounds and further work is now underway to identify the protein targets of this new class of anti-TB agents.

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.

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