scholarly journals Medicinal chemistry perspectives of 1,2,3,4-tetrahydroisoquinoline analogs – biological activities and SAR studies

RSC Advances ◽  
2021 ◽  
Vol 11 (20) ◽  
pp. 12254-12287
Author(s):  
Faheem ◽  
Banoth Karan Kumar ◽  
Kondapalli Venkata Gowri Chandra Sekhar ◽  
Subhash Chander ◽  
Selvaraj Kunjiappan ◽  
...  
Keyword(s):  
Medicinal Chemistry ◽  
Biological Activities ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Sar Studies ◽  
Structure Activity

This review provides critical insights into the biological activities and Structure–Activity Relationship (SAR) studies of tetrahydroisoquinoline (THIQ) analogs.

scholarly journals Recent Advances in Bioactive Flavonoid Hybrids Linked by 1,2,3-Triazole Ring Obtained by Click Chemistry

Molecules ◽  
2021 ◽  
Vol 27 (1) ◽  
pp. 230
Author(s):  
Daniela Pereira ◽  
Madalena Pinto ◽  
Marta Correia-da-Silva ◽  
Honorina Cidade
Keyword(s):  
Click Chemistry ◽  
Mechanism Of Action ◽  
Biological Activities ◽  
Triazole Ring ◽  
Pharmacokinetic Profile ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Antifouling Activity ◽  
Sar Studies ◽  
Structure Activity

As a result of the biological activities of natural flavonoids, several synthetic strategies aiming to obtain analogues with improved potency and/or pharmacokinetic profile have been developed. Since the triazole ring has been associated with several biological activities and metabolic stability, hybridization with a 1,2,3-triazole ring has been increasingly reported over the last years. The feasible synthesis through copper (I) catalyzed azide-alkyne cycloaddition (CuAAC) has allowed the accomplishment of several hybrids. Since 2017, almost 700 flavonoid hybrids conjugated with 1,2,3-triazole, including chalcones, flavones, flavanones and flavonols, among others, with antitumor, antimicrobial, antidiabetic, neuroprotective, anti-inflammatory, antioxidant, and antifouling activity have been reported. This review compiles the biological activities recently described for these hybrids, highlighting the mechanism of action and structure–activity relationship (SAR) studies.

Carbohydrazide analogues: a review of synthesis and biological activities

2021 ◽  
Vol 21 ◽  
Author(s):  
Ebuka Leonard Onyeyilim ◽  
Mercy Amarachi Ezeokonkwo ◽  
David Izuchukwu Ugwu ◽  
Chiamaka Peace Uzoewulu ◽  
Florence Uchenna Eze ◽  
...  
Keyword(s):  
Organic Chemistry ◽  
Inorganic Chemistry ◽  
Schiff Bases ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Important Class ◽  
Synthetic Route ◽  
Structure Activity

: Carbohydrazides and their Schiff bases are important class of heterocycles that are not only employed in the area of organic chemistry, but also have tremendous applications in physical and inorganic chemistry. A series of potential bioactive compounds, containing carbohydrazide functionality and their hydrazone derivatives have been synthesized and screened for antibacterial, anticancer, antifungal and anti-inflammatory etc. This brief review discloses some synthetic route to so many reported carbohydrazides, their Schiff bases, their biological activities and their structure activity relationship.

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.

scholarly journals INDANYL ANALOGS AS POTENTIAL ANTIMICROBIAL AGENTS

2018 ◽  
Vol 11 (5) ◽  
pp. 278 ◽  
Author(s):  
Sudip Kumar Mandal
Keyword(s):  
Antimicrobial Agents ◽  
Biological Activities ◽  
Antibacterial Activities ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Dilution Method ◽  
Pathogenic Microorganisms ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Structure Activity

 Objective: The wide variety of biological activities of different indane derivatives makes them an interesting moiety in the field of medicinal chemistry. The objective of the study was to identify and develop novel antimicrobial agents from indanyl analogs.Methods: Recently synthesized indanyl analogs (4a-c and 5a-o) were examined against various pathogenic microorganisms (Gram-positive and Gram-negative bacteria and fungi) using serial dilution method. These analogs were found to possess antibacterial and antifungal activities with minimum inhibitory concentration values ranging between 1.56 and 100 μg/mL.Results: The results revealed that the entire compounds showed mild-to-moderate antibacterial activities and moderate-to-excellent antifungal activities against the pathogenic microorganisms as compared to the standard drugs ciprofloxacin and fluconazole, respectively. Compounds 4a, 5a, 5b, 5d, 5e, 5i, and 5j exhibited antifungal activities superior to the reference drug.Conclusion: Based on the structure-activity relationship, it can conclude that the indan-3-oxo-1-acetic acid moiety is essential for the activities and lipophilic alkoxy substituents on indane ring have enhanced the biological activity. Further, structure-activity relationship studies of the compounds 4a, 5a, and 5b are needful to find the new lead as antimicrobial agent.

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