Fluoro-benzimidazole derivatives to cure Alzheimer’s disease: In-silico studies, synthesis, structure-activity relationship and in vivo evaluation for β secretase enzyme inhibition

2019 ◽  
Vol 88 ◽  
pp. 102936 ◽  
Author(s):  
Sayyad Ali ◽  
Muhammad Hassham Hassan Bin Asad ◽  
Soham Maity ◽  
Wahid Zada ◽  
Albert A. Rizvanov ◽  
...  
Keyword(s):  
Alzheimer’S Disease ◽  
Enzyme Inhibition ◽  
In Silico ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Benzimidazole Derivatives ◽  
In Vivo Evaluation ◽  
Structure Activity ◽  
In Silico Studies

Xanthone: Potential Acetylcholinesterase Inhibitor for Alzheimer's Disease Treatment

2021 ◽  
Vol 21 ◽  
Author(s):  
Vincentsia Vienna Vanessa ◽  
Siau Hui Mah
Keyword(s):  
Alzheimer’S Disease ◽  
Alzheimer's Disease ◽  
Neurodegenerative Disorder ◽  
Acetylcholinesterase Inhibitor ◽  
Structure Activity Relationship ◽  
Acetylcholinesterase Inhibition ◽  
Activity Relationship ◽  
Structure Activity ◽  
Hydrophobic Moiety

: Alzheimer's disease is a neurodegenerative disorder that results in progressive and irreversible central nervous system impairment, which has become one of the severe issues recently. The most successful approach of Alzheimer’s treatment is the administration of cholinesterase inhibitors to prevent the hydrolysis of acetylcholine and subsequently improve the cholinergic postsynaptic transmission. This review highlights a class of heterocycle, namely xanthone and its remarkable acetylcholinesterase inhibitory activities. Naturally occurring xanthones, including oxygenated, prenylated, pyrano and glycosylated xanthones exhibited promising inhibition effects towards acetylcholinesterase. Interestingly, synthetic xanthone derivatives with complex substituents such as alkyl, pyrrolidine, piperidine and morpholine have shown greater acetylcholinesterase inhibition activities. Structure-activity relationship of xanthones revealed that the type and position of substituent(s) attached to the xanthone moiety influenced their acetylcholinesterase inhibition activities where hydrophobic moiety will lead to an improved activity by contributing the π-π interactions, as well as the hydroxy substituent(s) by forming hydrogen-bond interactions. Thus, further studies including quantitative structure-activity relationship, in vivo and clinical validation studies are crucial for the development of xanthones into novel anti-Alzheimer's disease drugs.

Synthesis, Structure‐Activity Relationship and in silico Studies of Novel Pyrazolothiazole and Thiazolopyridine Derivatives as Prospective Antimicrobial and Anticancer Agents

2021 ◽  
Vol 6 (31) ◽  
pp. 7860-7872
Author(s):  
Ismail M. M. Othman ◽  
Mohamed A. M. Gad‐Elkareem ◽  
Hyam A. Radwan ◽  
Riadh Badraoui ◽  
Kaïss Aouadi ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
In Silico ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity ◽  
In Silico Studies

Structure–activity relationship study of dendritic polyglycerolamines for efficient siRNA transfection

RSC Advances ◽  
2015 ◽  
Vol 5 (96) ◽  
pp. 78760-78770 ◽  
Author(s):  
Fatemeh Sheikhi Mehrabadi ◽  
Ole Hirsch ◽  
Reiner Zeisig ◽  
Paola Posocco ◽  
Erik Laurini ◽  
...  
Keyword(s):  
In Silico ◽  
Gene Transfection ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Sirna Transfection ◽  
Structure Activity ◽  
Relationship Study

Structure–activity relationship studies were performed through in vitro, in silico, and in vivo analysis in order to evaluate the gene transfection potential of dendritic polyglycerolamines with different amine loadings.

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