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.

Synthesis and biological activities of 2-aminophenol-based Schiff bases and their structure–activity relationship

2015 ◽  
Vol 25 (1) ◽  
pp. 109-115 ◽  
Author(s):  
Muhammad Aslam ◽  
Itrat Anis ◽  
Rashad Mehmood ◽  
Lubna Iqbal ◽  
Samina Iqbal ◽  
...  
Keyword(s):  
Schiff Bases ◽  
Biological Activities ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Structure Activity

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.

scholarly journals SYNTHESIS, CHARACTERIZATION, QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP, DOCKING, ANTIBACTERIAL ACTIVITY, AND BRINE SHRIMP LETHAL STUDIES ON L-PHENYLALANINE SCHIFF BASES

2016 ◽  
Vol 9 (9) ◽  
pp. 203
Author(s):  
Easwaramoorthi Deivanayagam ◽  
Jayaprakash R ◽  
Aroj Kumar Sha ◽  
Hemalatha S
Keyword(s):  
Antibacterial Activity ◽  
Schiff Base ◽  
Schiff Bases ◽  
Brine Shrimp ◽  
Quantitative Structure Activity Relationship ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Hydroxyl Group ◽  
Quantitative Structure ◽  
Structure Activity

ABSTRACTObjective: Aim of this work is to synthesize and characterization of the hydroxyl group the hydroxyl group substituted L-phenylalanine Schiff basesto compare their predicted quantitative structure-activity relationship (QSAR) and molecular docking against Escherichia coli protein ZipA (1s1j)outcomes with the antibacterial activity and brine shrimp lethal assay (BSLA) results.Methods: The Schiff bases of L-Phenylalanine were synthesized by the simple condensation reaction using methanol, water in 2:1 ratio at reflux andwere characterized by spectral techniques. QSAR parameters of the Schiff bases were predicted using java-based online and offline tools. Moleculardocking carried through online mcule server and CLC Drug Discovery Workbench 3. Antibacterial activity and toxicity studies were conducted usingbroth dilution and brine shrimp lethal assay methods, respectively.Results: The Schiff bases fulfilled the QSAR drug-likeness parameters and showed the docking score between −6.8 and −6.0 Kcal/mol which arehigher than amoxilicillin and gentamicin like standard drugs. They also possess good inhibition for urinary tract infection causing E. coli bacteria,and minimum inhibitory concentrations (MIC) exists between 3.25 and 5.25 μg/ml. The brine shrimp lethal concentration for 50% mortality [LC50])between 58.73 and 135.6 μg/ml.Conclusion: Para, meta and 2,4 hydroxyl substituted Schiff bases exhibited good inhibition against Gram-negative E. coli bacteria at low concentrationand the MIC exists below the LC50 value. The Schiff base showed high drug score, high docking score, and low toxicity than other Schiff base. Dockingscore, high inhibition, low clogP, low MICKeywords: L-phenylalanine, Schiff base, Quantitative structure-activity relationship, Docking, Antibacterial, Lethal concentration for 50% mortality.

A Review on Anticancer Potentials of Benzothiazole Derivatives

2020 ◽  
Vol 20 (1) ◽  
pp. 12-23 ◽  
Author(s):  
Nandini Pathak ◽  
Ekta Rathi ◽  
Nitesh Kumar ◽  
Suvarna G. Kini ◽  
C. Mallikarjuna Rao
Keyword(s):  
Biological Activities ◽  
Cancer Cell Line ◽  
Structure Activity Relationship ◽  
Potential Effect ◽  
Activity Relationship ◽  
Oxygen Species ◽  
Benzothiazole Derivatives ◽  
Structure Activity ◽  
Wide Range ◽  
Recent Trends

: 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.

Structure-activity relationship of the pro- and anticoagulant effects of Fucus vesiculosus fucoidan

2014 ◽  
Vol 111 (03) ◽  
pp. 429-437 ◽  
Author(s):  
Cong Jiang ◽  
Sabine Knappe ◽  
Sabrina Reutterer ◽  
Christina Szabo ◽  
Michael Dockal ◽  
...  
Keyword(s):  
Charge Density ◽  
Biological Activities ◽  
Brown Seaweed ◽  
Structure Activity Relationship ◽  
Structural Features ◽  
Fucus Vesiculosus ◽  
Factor Ix ◽  
Activity Relationship ◽  
Structure Activity ◽  
The Impact

SummaryFucoidan is a highly complex sulfated polysaccharide commonly extracted from brown seaweed. In addition to their many biological activities, fucoidans have recently been demonstrated to inhibit or increase coagulation at different concentration ranges. Their structural features, i.e. molecular weight (Mw), Mw distribution, degree of sulfation, monosaccharide composition, and different linkages, are known to affect these activities. Therefore, structure-activity relationship (SAR) analysis of fucoidan is crucial for its potential use as a procoagulant. In this study, Fucus vesiculosus (F.v.) fucoidan was fractionated by charge and size as well as over- and desulfated to different degrees to yield preparations with various structural properties. The fractions’ pro- and anticoagulant activities were assessed by calibrated automated thrombography (CAT) and activated partial thromboplastin time (aPTT) assays. Binding to and inhibition of the anticoagulant protein tissue factor pathway inhibitor (TFPI) and the ability to activate coagulation via the contact pathway were also investigated. This paper discusses the impact of charge density, size, and sugar composition on fucoidan’s pro- and anticoagulant activities. Fucoidan requires a minimal charge density of 0.5 sulfates per sugar unit and a size of 70 sugar units to demonstrate desired procoagulant activities for improvement of haemostasis in factor VIII/factor IX-deficient plasma.

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