Microwave-assisted synthesis of new sulfonyl hydrazones, screening of biological activities and investigation of structure–activity relationship

2016 ◽  
Vol 25 (8) ◽  
pp. 1590-1607 ◽  
Author(s):  
Nurcan Karaman ◽  
Emine Elçin Oruç-Emre ◽  
Yusuf Sıcak ◽  
Berna Çatıkkaş ◽  
Ayşegül Karaküçük-İyidoğan ◽  
...  
RSC Advances ◽  
2018 ◽  
Vol 8 (35) ◽  
pp. 19883-19893 ◽  
Author(s):  
Fei Ye ◽  
Peng Ma ◽  
Yue Zhai ◽  
Fei Yang ◽  
Shuang Gao ◽  
...  

Based on the structure–activity relationship and active substructure combination, a novel class of substituted 2-phenyl-2-cyclohexanedione enol ester derivatives was designed for use as potential herbicide safeners.


Author(s):  
Ebuka Leonard Onyeyilim ◽  
Mercy Amarachi Ezeokonkwo ◽  
David Izuchukwu Ugwu ◽  
Chiamaka Peace Uzoewulu ◽  
Florence Uchenna Eze ◽  
...  

: 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.


Author(s):  
Sudip Kumar Mandal

 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.


2020 ◽  
Vol 20 (1) ◽  
pp. 12-23 ◽  
Author(s):  
Nandini Pathak ◽  
Ekta Rathi ◽  
Nitesh Kumar ◽  
Suvarna G. Kini ◽  
C. Mallikarjuna Rao

: Benzothiazole is an organic compound bearing a heterocyclic nucleus (thiazole) which imparts a broad spectrum of biological activities to it. The significant and potent activity of benzothiazole moiety influenced distinctively by nature and position of substitutions. This review summarizes the effect of various substituents in recent trends and approaches to design and develop novel benzothiazole derivatives for anticancer potential in different cell lines by interpreting the Structure- Activity Relationship (SAR) and mechanism of action of a wide range of derivatives. The list of derivatives is categorized into different groups and reviewed for their anticancer activity. The structure-activity relationship for the various derivatives revealed an excellent understanding of benzothiazole moiety in the field of cancer therapy against different cancer cell line. Data obtained from the various articles showed the potential effect of benzothiazole moiety and its derivatives to produce the peculiar and significant lead compound. The important anticancer mechanisms found are tyrosine kinase inhibition, topoisomerase inhibition and induction of apoptosis by Reactive Oxygen Species (ROS) activation. Therefore, the design and development of novel benzothiazole have broad scope in cancer chemotherapy.


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