From Type I to Type II: Design, Synthesis, and Characterization of Potent Pyrazin-2-ones as DFG-Out Inhibitors of PDGFRβ

ChemMedChem ◽  
2016 ◽  
Vol 11 (24) ◽  
pp. 2664-2674 ◽  
Author(s):  
Eugen Bethke ◽  
Boris Pinchuk ◽  
Christian Renn ◽  
Lydia Witt ◽  
Joachim Schlosser ◽  
...  
Lubricants ◽  
2019 ◽  
Vol 7 (12) ◽  
pp. 110 ◽  
Author(s):  
Quan Tran ◽  
Matt Fuka ◽  
Maharshi Dey ◽  
Surojit Gupta

We report the synthesis and characterization of two different types of Ni-based laminated composites (Types I and II). In Type-I composites, layers of Ni and Ti3SiC2 (Ni–Ti3SiC2) were interleaved with Ni, whereas in Type-II composites, Ni–Ti3SiC2 layers were interleaved with Al and Ni. The laminate thickness and Ti3SiC2 content in the individual Ni–Ti3SiC2 layers were systematically varied in both the composites. Detailed SEM studies showed that Ti3SiC2 particulates are well distributed in the Ni-matrix with little or no interfacial reactions with interparticle porosity. However, there were interfacial reactions between Ni and Al in Type II composites. In general, Type I multilayered composites had higher ultimate compressive strength (UCS) in parallel orientation as compared to perpendicular orientation (layers are aligned parallel or perpendicular to the wear surface then it will be referred to as parallel or perpendicular orientation). Comparatively, in Type II composites, the UCS was greater in perpendicular orientation as compared to parallel due to the presence of Al layers as bonding layers. Both the composite designs showed triboactive behavior against alumina disks and sensitivity to laminate thickness and orientation. In Type-I composites, the decrease in µ and wear rate (WR) with laminate thickness was more pronounced in the perpendicular orientation as compared to the parallel orientation. Comparatively, Ni–Ti3SiC2/Al/Ni composites showed that the parallel orientation was more effective in enhancing the triboactive performance. SEM analysis of tribosurfaces showed signs of triboxidation and abrasion, which led to the formation of O-rich tribofilms.


2021 ◽  
Author(s):  
Teng Chi ◽  
Siddhartha Akkiraju ◽  
Zihao Liang ◽  
Ying Tan ◽  
Ho Joong Kim ◽  
...  

We document the design, synthesis, and characterization of the first low glass transition temperature, n-type (i.e., preferentially-reduced) radical polymer.


ChemMedChem ◽  
2020 ◽  
Vol 15 (13) ◽  
pp. 1150-1162
Author(s):  
Yu Lin ◽  
Zhanhui Li ◽  
Haikuo Ma ◽  
Yujie Wang ◽  
Xu Wang ◽  
...  

2011 ◽  
Vol 47 (31) ◽  
pp. 8955 ◽  
Author(s):  
Giuseppe Lamanna ◽  
Julie Russier ◽  
Cécilia Ménard-Moyon ◽  
Alberto Bianco

2013 ◽  
Vol 65 ◽  
pp. 60-69 ◽  
Author(s):  
Sashikanth Banappagari ◽  
Alecia McCall ◽  
Krystal Fontenot ◽  
M. Graca H. Vicente ◽  
Amit Gujar ◽  
...  

Author(s):  
SURENDRA BABU LAGU ◽  
RAJENDRA PRASAD YEJELLA

Objective: Investigation, the series of newer 2‐amino-pyridine‐3‐carbonitrile and 2‐amino-4H-pyran‐3‐carbonitrile derivative were synthesized and evaluated antimicrobial activities and antioxidant activity. Methods: Novel synthesized chalcones were further condensation to give 2-amino-3-cyanopyridine and 2-amino-3-cyanopyrans in the presence of malononitrile, pyridine, and ammonia acetate. The product is characterized by conventional and instrumental methods. Pyridine and 4-H-Pyran and their analogs occupy prime position due to their diverse applications. Results: The compounds A3C and B3C exhibited marked zone of inhibition with 30.02±0.02 mm and 29.06±0.01 mm, respectively. Docking studies suggested possible interactions with dihydrofolic reductase 4 with 9.15 and −9.67 kcal/mol, respectively. The IC50 30.28±0.01 exhibited A3C by 2,2-diphenylpicrylhydrazyl methods which is better among the series. The 2-amino-3-cyanopyridine derivatives were found good activity than 2-amino-3-cyanopyrane derivative. Among all synthesized compounds few having potent activity and some are near to the standard. Conclusion: Antimicrobial activity and antioxidant of the newly synthesized pyrans and pyridines derivatives will definitely inspire future researchers for the preparation of new analogs.


2018 ◽  
Vol 9 (12) ◽  
pp. 1223-1229 ◽  
Author(s):  
Carolyn N. Paulson ◽  
Xianghong Guan ◽  
Alex M. Ayoub ◽  
Alice Chan ◽  
Rezaul M. Karim ◽  
...  

2006 ◽  
Vol 39 (13) ◽  
pp. 4317-4326 ◽  
Author(s):  
Cheng Zhang ◽  
Soobum Choi ◽  
James Haliburton ◽  
Taina Cleveland ◽  
Rui Li ◽  
...  

Sign in / Sign up

Export Citation Format

Share Document