scholarly journals Synthesis, applications and Structure-Activity Relationship (SAR) of cinnamic acid derivatives: a review

2021 ◽  
Vol 10 (1) ◽  
pp. e28010111691
Author(s):  
Saraliny Bezerra França ◽  
Paulo Ricardo dos Santos Correia ◽  
Ilton Barros Daltro de Castro ◽  
Edeildo Ferreira da Silva Júnior ◽  
Maria Ester de Sá Barreto Barros ◽  
...  
Keyword(s):  
Cinnamic Acid ◽  
Therapeutic Potential ◽  
Structure Activity Relationship ◽  
Bioactive Molecules ◽  
Activity Relationship ◽  
Cinnamic Acid Derivatives ◽  
Structure Activity ◽  
Synthetic Routes ◽  
Synthetic Methodologies ◽  
Pharmacologically Active

The article aims to analyze the progress of the evolution of cinnamic acid derivatives through a bibliographic review, describing the main synthetic routes in obtaining this class, as well as remarkable biological applications and application of the structure-activity relationship (SAR) as a strategy for design pharmacologically active molecules. The methodology used consists of reading and analyzing articles, whose approach is descriptive, with data being collected regarding the therapeutic potential of derivatives of cinnamic acid and its relationship with structural scaffolding, as well as the most widely used synthetic approaches. As a result, it was observed that cinnamic acid and its derivatives from natural sources can be synthesized in appreciable quantities with varied synthetic routes, as well as being candidates for therapeutic agents, since they have several therapeutic applications against diabetes, infectious and degenerative diseases, among others, in addition to presenting activity such as pest control, which has attracted the attention of academic and industrial researchers. These compounds are highly versatile since their activity is intrinsically associated with the mode of interaction between the structure and its molecular target. However, in nature they are obtained in small quantities, therefore, the development of new approaches of synthetic methodologies to obtain such compounds in substantial quantities and linked to medicinal chemistry can contribute to the development of very effective bioactive molecules in comparison with their precursors.

Trans-3-Phenyl-2-Propenoic Acid (Cinnamic Acid) Derivatives: Structure-Activity Relationship as Hepatoprotective Agents

2007 ◽  
Vol 3 (5) ◽  
pp. 475-479 ◽  
Author(s):  
Eduardo Fernandez-Martinez ◽  
Rosa Bobadilla ◽  
Martha Morales-Rios ◽  
Pablo Muriel ◽  
Victor Perez-Alvarez
Keyword(s):  
Cinnamic Acid ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Cinnamic Acid Derivatives ◽  
Structure Activity ◽  
Propenoic Acid ◽  
Hepatoprotective Agents

Review: Studies on the Synthesis of Quinolone Derivatives with Their Antibacterial Activity (Part 1)

2020 ◽  
Vol 24 (8) ◽  
pp. 817-854
Author(s):  
Anil Kumar ◽  
Nishtha Saxena ◽  
Arti Mehrotra ◽  
Nivedita Srivastava
Keyword(s):  
Antibacterial Activity ◽  
Antibacterial Properties ◽  
Structure Activity Relationship ◽  
New Drugs ◽  
Activity Relationship ◽  
Structure Activity ◽  
Medicinal Properties ◽  
Synthetic Routes ◽  
Quinolone Derivatives

Quinolone derivatives have attracted considerable attention due to their medicinal properties. This review covers many synthetic routes of quinolones preparation with their antibacterial properties. Detailed study with structure-activity relationship among quinolone derivatives will be helpful in designing new drugs in this field.

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.

scholarly journals Antioxidant, Cytotoxic, Genotoxic, and DNA-Protective Potential of 2,3-Substituted Quinazolinones: Structure—Activity Relationship Study

2021 ◽  
Vol 22 (2) ◽  
pp. 610
Author(s):  
Jana Hricovíniová ◽  
Zuzana Hricovíniová ◽  
Katarína Kozics
Keyword(s):  
Radical Scavenging ◽  
Reducing Power ◽  
Structure Activity Relationship ◽  
Dna Lesions ◽  
Activity Relationship ◽  
Antioxidant Compounds ◽  
Substitution Pattern ◽  
Structure Activity ◽  
Pharmacologically Active ◽  
Th 1

The evaluation of antioxidant compounds that counteract the mutagenic effects caused by the direct action of reactive oxygen species on DNA molecule is of considerable interest. Therefore, a series of 2,3-substituted quinazolinone derivatives (Q1–Q8) were investigated by different assays, and the relationship between their biological properties and chemical structure was examined. Genotoxicity and the potential DNA-protective effects of Q1–Q8 were evaluated by comet assay and DNA topology assay. Antioxidant activity was examined by DPPH-radical-scavenging, reducing-power, and total antioxidant status (TAS) assays. The cytotoxic effect of compounds was assessed in human renal epithelial cells (TH-1) and renal carcinoma cells (Caki-1) by MTT assay. Analysis of the structure–activity relationship disclosed significant differences in the activity depending on the substitution pattern. Derivatives Q5–Q8, bearing electron-donating moieties, were the most potent members of this series. Compounds were not genotoxic and considerably decreased the levels of DNA lesions induced by oxidants (H2O2, Fe2+ ions). Furthermore, compounds exhibited higher cytotoxicity in Caki-1 compared to that in TH-1 cells. Substantial antioxidant effect and DNA-protectivity along with the absence of genotoxicity suggested that the studied quinazolinones might represent potential model structures for the development of pharmacologically active agents.

scholarly journals Synthesis and leishmanicidal activity of cinnamic acid esters: structure–activity relationship

2013 ◽  
Vol 23 (3) ◽  
pp. 1378-1386 ◽  
Author(s):  
Elver Otero ◽  
Sara M. Robledo ◽  
Santiago Díaz ◽  
Miguel Carda ◽  
Diana Muñoz ◽  
...  
Keyword(s):  
Cinnamic Acid ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Leishmanicidal Activity ◽  
Structure Activity ◽  
Acid Esters

scholarly journals Synthetic and therapeutic potential of 4-thiazolidinone and its analogs

2021 ◽  
pp. 119-138 ◽  
Author(s):  
Neetu Agrawal
Keyword(s):  
Therapeutic Agent ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
The Past ◽  
Structure Activity ◽  
Potent Therapeutic Agent

Past researches on 4-thiazolidinone nucleus have revealed the prominent potential of derivatives containing this nucleus to be developed as a potent therapeutic agent. Because of these biological activities, their structure-activity relationship has created an interest for medicinal chemists leading to the discovery of a number of lead molecules. This review highlights the routes for its synthesis and summarizes the past and recent studies on its biological activities to guide the medicinal chemists working on this nucleus in the development of clinically viable drugs.

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