Molecular design, synthesis, and structure–Activity relationships leading to the potent and selective p56lck inhibitor BMS-243117

2003 ◽  
Vol 13 (13) ◽  
pp. 2145-2149 ◽  
Author(s):  
Jagabandhu Das ◽  
James Lin ◽  
Robert V. Moquin ◽  
Zhongqi Shen ◽  
Steven H. Spergel ◽  
...  
Keyword(s):  
Molecular Design ◽  
Design Synthesis ◽  
Structure Activity Relationships ◽  
Structure Activity

Development of Novel Glitazones as Antidiabetic Agents: Molecular Design, Synthesis, Evaluation of Glucose Uptake Activity and SAR Studies

2020 ◽  
Vol 17 (7) ◽  
pp. 840-849
Author(s):  
Mahendra Gowdru Srinivas ◽  
Prabitha Prabhakaran ◽  
Subhankar Probhat Mandal ◽  
Yuvaraj Sivamani ◽  
Pranesh Guddur ◽  
...  
Keyword(s):  
Glucose Uptake ◽  
Molecular Design ◽  
Docking Studies ◽  
Antidiabetic Activity ◽  
Design Synthesis ◽  
In Silico Docking ◽  
Ppar Γ ◽  
Sar Studies ◽  
Structure Activity ◽  
Uptake Activity

Background: Thiazolidinediones and its bioisostere, namely, rhodanines have become ubiquitous class of heterocyclic compounds in drug design and discovery. In the present study, as part of molecular design, a series of novel glitazones that are feasible to synthesize in our laboratory were subjected to docking studies against PPAR-γ receptor for their selection. Methods and Results: As part of the synthesis of selected twelve glitazones, the core moiety, pyridine incorporated rhodanine was synthesized via dithiocarbamate. Later, a series of glitazones were prepared via Knovenageal condensation. In silico docking studies were performed against PPARγ protein (2PRG). The titled compounds were investigated for their cytotoxic activity against 3T3-L1 cells to identify the cytotoxicity window of the glitazones. Further, within the cytotoxicity window, glitazones were screened for glucose uptake activity against L6 cells to assess their possible antidiabetic activity. Conclusion: Based on the glucose uptake results, structure activity relationships are drawn for the title compounds.

Design, Synthesis, and Structure−Activity Relationships of Benzophenone-Based Tetraamides as Novel Antibacterial Agents

2009 ◽  
Vol 52 (16) ◽  
pp. 5020-5031 ◽  
Author(s):  
Sunil K. Vooturi ◽  
Chrissy M. Cheung ◽  
Michael J. Rybak ◽  
Steven M. Firestine
Keyword(s):  
Antibacterial Agents ◽  
Design Synthesis ◽  
Structure Activity Relationships ◽  
Structure Activity
Sign in / Sign up

Export Citation Format

Share Document