Design, synthesis, and characterization of some new benzimidazole derivatives and biological evaluation

2020 ◽  
Vol 57 (5) ◽  
pp. 2234-2242
Author(s):  
Hakan Bektaş ◽  
Bahar B. Sökmen ◽  
Sinem Aydın ◽  
Emre Menteşe ◽  
Adile Bektaş ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Synthesis And Characterization ◽  
Benzimidazole Derivatives ◽  
Design Synthesis

scholarly journals New 4-Aminoproline-Based Small Molecule Cyclopeptidomimetics as Potential Modulators of α4β1 Integrin

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 6066
Author(s):  
Andrea Sartori ◽  
Kelly Bugatti ◽  
Elisabetta Portioli ◽  
Monica Baiula ◽  
Irene Casamassima ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Jurkat Cells ◽  
Synthesis And Characterization ◽  
Primary Role ◽  
Agonist Activity ◽  
Design Synthesis ◽  
Molecular Modeling Studies ◽  
New Compounds ◽  
Integrin Family

Integrin α4β1 belongs to the leukocyte integrin family and represents a therapeutic target of relevant interest given its primary role in mediating inflammation, autoimmune pathologies and cancer-related diseases. The focus of the present work is the design, synthesis and characterization of new peptidomimetic compounds that are potentially able to recognize α4β1 integrin and interfere with its function. To this aim, a collection of seven new cyclic peptidomimetics possessing both a 4-aminoproline (Amp) core scaffold grafted onto key α4β1-recognizing sequences and the (2-methylphenyl)ureido-phenylacetyl (MPUPA) appendage, was designed, with the support of molecular modeling studies. The new compounds were synthesized through SPPS procedures followed by in-solution cyclization maneuvers. The biological evaluation of the new cyclic ligands in cell adhesion assays on Jurkat cells revealed promising submicromolar agonist activity in one compound, namely, the c[Amp(MPUPA)Val-Asp-Leu] cyclopeptide. Further investigations will be necessary to complete the characterization of this class of compounds.

scholarly journals Design of an n-type low glass transition temperature radical polymer

2021 ◽  
Author(s):  
Teng Chi ◽  
Siddhartha Akkiraju ◽  
Zihao Liang ◽  
Ying Tan ◽  
Ho Joong Kim ◽  
...  
Keyword(s):  
Glass Transition ◽  
Transition Temperature ◽  
Glass Transition Temperature ◽  
Synthesis And Characterization ◽  
Design Synthesis

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

Design, Synthesis, and Characterization of Novel CXCR4 Antagonists Featuring Cyclic Amines

ChemMedChem ◽  
2020 ◽  
Vol 15 (13) ◽  
pp. 1150-1162
Author(s):  
Yu Lin ◽  
Zhanhui Li ◽  
Haikuo Ma ◽  
Yujie Wang ◽  
Xu Wang ◽  
...  
Keyword(s):  
Synthesis And Characterization ◽  
Design Synthesis ◽  
Cyclic Amines ◽  
Cxcr4 Antagonists

HYDRAmers: design, synthesis and characterization of different generation novel Hydra-like dendrons based on multifunctionalized adamantane

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

scholarly journals Design, synthesis and characterization of peptidomimetic conjugate of BODIPY targeting HER2 protein extracellular domain

2013 ◽  
Vol 65 ◽  
pp. 60-69 ◽  
Author(s):  
Sashikanth Banappagari ◽  
Alecia McCall ◽  
Krystal Fontenot ◽  
M. Graca H. Vicente ◽  
Amit Gujar ◽  
...  
Keyword(s):  
Extracellular Domain ◽  
Synthesis And Characterization ◽  
Design Synthesis ◽  
Her2 Protein

DESIGN, SYNTHESIS, AND CHARACTERIZATION OF THE SOME NOVEL 2‐AMINO-PYRIDINE‐3‐ CARBONITRILE AND 2‐AMINO-4H-PYRAN‐3‐CARBONITRILE DERIVATIVES AGAINST ANTIMICROBIAL ACTIVITY AND ANTIOXIDANT ACTIVITY

2020 ◽  
pp. 125-134
Author(s):  
SURENDRA BABU LAGU ◽  
RAJENDRA PRASAD YEJELLA
Keyword(s):  
Antimicrobial Activity ◽  
Antioxidant Activity ◽  
Antimicrobial Activities ◽  
Docking Studies ◽  
Synthesis And Characterization ◽  
Zone Of Inhibition ◽  
Design Synthesis ◽  
Instrumental Methods ◽  
Objective Investigation

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.

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