N-(5-acetyl-4-methylthiazol-2-yl)arylamide derivatives as multi-target-directed ligands: design, synthesis, biochemical evaluation and computational analysis

2022 ◽  
Vol 134 (1) ◽  
Author(s):  
Rabail Ujan ◽  
Hafiz Mohammad Kashif Mahmood ◽  
Pervaiz Ali Channar ◽  
Syeda Abida Ejaz ◽  
Shomaila Saeed ◽  
...  
Keyword(s):  
Computational Analysis ◽  
Design Synthesis ◽  
Biochemical Evaluation

Ligand-based design, synthesis and biochemical evaluation of potent and selective inhibitors of Schistosoma mansoni dihydroorotate dehydrogenase

2019 ◽  
Vol 167 ◽  
pp. 357-366 ◽  
Author(s):  
Felipe A. Calil ◽  
Juliana S. David ◽  
Estela R.C. Chiappetta ◽  
Fernando Fumagalli ◽  
Rodrigo B. Mello ◽  
...  
Keyword(s):  
Schistosoma Mansoni ◽  
Dihydroorotate Dehydrogenase ◽  
Selective Inhibitors ◽  
Design Synthesis ◽  
Biochemical Evaluation

Design, synthesis and biochemical evaluation of novel multi-target inhibitors as potential anti-Parkinson agents

2018 ◽  
Vol 143 ◽  
pp. 1543-1552 ◽  
Author(s):  
Simone Carradori ◽  
Francesco Ortuso ◽  
Anél Petzer ◽  
Donatella Bagetta ◽  
Celeste De Monte ◽  
...  
Keyword(s):  
Design Synthesis ◽  
Biochemical Evaluation

Design, synthesis and computational analysis of novel acridine-(sulfadiazine/sulfathiazole) hybrids as antibacterial agents

2019 ◽  
Vol 1186 ◽  
pp. 39-49 ◽  
Author(s):  
Miyase Gözde Gündüz ◽  
Muhammad Nawaz Tahir ◽  
Stevan Armaković ◽  
Ceren Özkul Koçak ◽  
Sanja J. Armaković
Keyword(s):  
Antibacterial Agents ◽  
Computational Analysis ◽  
Design Synthesis

Design, synthesis, and biochemical evaluation of novel αvβ3 integrin ligands

2004 ◽  
Vol 14 (17) ◽  
pp. 4553-4555 ◽  
Author(s):  
Juan Jose Marugan ◽  
Kristin D Haslow ◽  
Carl Crysler
Keyword(s):  
Αvβ3 Integrin ◽  
Design Synthesis ◽  
Biochemical Evaluation ◽  
Integrin Ligands

scholarly journals Combining Chalcones with Donepezil to Inhibit Both Cholinesterases and Aβ Fibril Assembly

Molecules ◽  
2019 ◽  
Vol 25 (1) ◽  
pp. 77 ◽  
Author(s):  
Nishad Thamban Chandrika ◽  
Marina Y. Fosso ◽  
Oleg V. Tsodikov ◽  
Harry LeVine ◽  
Sylvie Garneau-Tsodikova
Keyword(s):  
Binding Site ◽  
Amyloid Β ◽  
Brain Disorder ◽  
Pittsburgh Compound B ◽  
Design Synthesis ◽  
Aβ Peptides ◽  
Limited Availability ◽  
Bche Activity ◽  
Biochemical Evaluation ◽  
The Relationship

The fact that the number of people with Alzheimer’s disease is increasing, combined with the limited availability of drugs for its treatment, emphasize the need for the development of novel effective therapeutics for treating this brain disorder. Herein, we focus on generating 12 chalcone-donepezil hybrids, with the goal of simultaneously targeting amyloid-β (Aβ) peptides as well as cholinesterases (i.e., acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)). We present the design, synthesis, and biochemical evaluation of these two series of novel 1,3-chalcone-donepezil (15a–15f) or 1,4-chalcone-donepezil (16a–16f) hybrids. We evaluate the relationship between their structures and their ability to inhibit AChE/BChE activity as well as their ability to bind Aβ peptides. We show that several of these novel chalcone-donepezil hybrids can successfully inhibit AChE/BChE as well as the assembly of N-biotinylated Aβ(1–42) oligomers. We also demonstrate that the Aβ binding site of these hybrids differs from that of Pittsburgh Compound B (PIB).

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