2,4-Disubstituted quinazolines as amyloid-β aggregation inhibitors with dual cholinesterase inhibition and antioxidant properties: Development and structure-activity relationship (SAR) studies

2017 ◽  
Vol 126 ◽  
pp. 823-843 ◽  
Author(s):  
Tarek Mohamed ◽  
Praveen P.N. Rao
Keyword(s):  
Antioxidant Properties ◽  
Amyloid Β ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Cholinesterase Inhibition ◽  
Sar Studies ◽  
Structure Activity ◽  
Aggregation Inhibitors

scholarly journals Flavonoids from the Genus Euphorbia: Isolation, Structure, Pharmacological Activities and Structure–Activity Relationships

2021 ◽  
Vol 14 (5) ◽  
pp. 428
Author(s):  
Douglas Kemboi Magozwi ◽  
Mmabatho Dinala ◽  
Nthabiseng Mokwana ◽  
Xavier Siwe-Noundou ◽  
Rui W. M. Krause ◽  
...  
Keyword(s):  
Therapeutic Potential ◽  
Antioxidant Properties ◽  
Structure Activity Relationship ◽  
Biological Properties ◽  
Therapeutic Agents ◽  
Skeletal Structure ◽  
Activity Relationship ◽  
Hydroxyl Groups ◽  
Structure Activity ◽  
Review Reports

Plants of the genus Euphorbia are widely distributed across temperate, tropical and subtropical regions of South America, Asia and Africa with established Ayurvedic, Chinese and Malay ethnomedical records. The present review reports the isolation, occurrence, phytochemistry, biological properties, therapeutic potential and structure–activity relationship of Euphorbia flavonoids for the period covering 2000–2020, while identifying potential areas for future studies aimed at development of new therapeutic agents from these plants. The findings suggest that the extracts and isolated flavonoids possess anticancer, antiproliferative, antimalarial, antibacterial, anti-venom, anti-inflammatory, anti-hepatitis and antioxidant properties and have different mechanisms of action against cancer cells. Of the investigated species, over 80 different types of flavonoids have been isolated to date. Most of the isolated flavonoids were flavonols and comprised simple O-substitution patterns, C-methylation and prenylation. Others had a glycoside, glycosidic linkages and a carbohydrate attached at either C-3 or C-7, and were designated as d-glucose, l-rhamnose or glucorhamnose. The structure–activity relationship studies showed that methylation of the hydroxyl groups on C-3 or C-7 reduces the activities while glycosylation loses the activity and that the parent skeletal structure is essential in retaining the activity. These constituents can therefore offer potential alternative scaffolds towards development of new Euphorbia-based therapeutic agents.

Design, Synthesis, and Structure–Activity Relationship ofN-Arylnaphthylamine Derivatives as Amyloid Aggregation Inhibitors

2012 ◽  
Vol 55 (19) ◽  
pp. 8538-8548 ◽  
Author(s):  
Roberto Di Santo ◽  
Roberta Costi ◽  
Giuliana Cuzzucoli Crucitti ◽  
Luca Pescatori ◽  
Federica Rosi ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Amyloid Aggregation ◽  
Design Synthesis ◽  
Structure Activity ◽  
Aggregation Inhibitors

scholarly journals Potent α-amino-β-lactam carbamic acid ester as NAAA inhibitors. Synthesis and structure–activity relationship (SAR) studies

2016 ◽  
Vol 111 ◽  
pp. 138-159 ◽  
Author(s):  
Andrea Nuzzi ◽  
Annalisa Fiasella ◽  
Jose Antonio Ortega ◽  
Chiara Pagliuca ◽  
Stefano Ponzano ◽  
...  
Keyword(s):  
Acid Ester ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Carbamic Acid ◽  
Sar Studies ◽  
Structure Activity

Structure–activity relationship of novel low-generation dendrimers for gene delivery

2018 ◽  
Vol 16 (42) ◽  
pp. 7833-7842 ◽  
Author(s):  
Yong-Guang Gao ◽  
Xiao Lin ◽  
Kai Dang ◽  
Shan-Feng Jiang ◽  
Ye Tian ◽  
...  
Keyword(s):  
Gene Delivery ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Sar Studies ◽  
Structure Activity ◽  
Gene Vectors ◽  
Relationship Of

Structure–activity relationship (SAR) studies are very critical to design ideal gene vectors for gene delivery.

Sign in / Sign up

Export Citation Format

Share Document