O ‐Glycoside quercetin derivatives: Biological activities, mechanisms of action, and structure–activity relationship for drug design, a review

: 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.

Download Full-text

INDANYL ANALOGS AS POTENTIAL ANTIMICROBIAL AGENTS

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i5.24635 ◽

2018 ◽

Vol 11 (5) ◽

pp. 278 ◽

Cited By ~ 1

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.

Download Full-text

A Review on Anticancer Potentials of Benzothiazole Derivatives

Mini-Reviews in Medicinal Chemistry ◽

10.2174/1389557519666190617153213 ◽

2020 ◽

Vol 20 (1) ◽

pp. 12-23 ◽

Cited By ~ 4

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.

Download Full-text

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

Medicinal Chemistry Research ◽

10.1007/s00044-015-1468-8 ◽

2015 ◽

Vol 25 (1) ◽

pp. 109-115 ◽

Cited By ~ 3

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

Download Full-text

Synthesis, Biological Activities, and Quantitative Structure–Activity Relationship (QSAR) Study of Novel Camptothecin Analogues

Molecules ◽

10.3390/molecules20058634 ◽

2015 ◽

Vol 20 (5) ◽

pp. 8634-8653 ◽

Cited By ~ 2

Author(s):

Dan Wu ◽

Shao-Yong Zhang ◽

Ying-Qian Liu ◽

Xiao-Bing Wu ◽

Gao-Xiang Zhu ◽

...

Keyword(s):

Biological Activities ◽

Quantitative Structure Activity Relationship ◽

Structure Activity Relationship ◽

Activity Relationship ◽

Quantitative Structure ◽

Qsar Study ◽

Structure Activity ◽

Camptothecin Analogues

Download Full-text

The disposition of diphenhydramine and four of its analogues in rabbits and implication for structure-activity relationship studies in drug design

Biopharmaceutics & Drug Disposition ◽

10.1002/bdd.2510030308 ◽

1982 ◽

Vol 3 (3) ◽

pp. 255-265 ◽

Cited By ~ 5

Author(s):

Rosalind Parry ◽

R. T. Calvert

Keyword(s):

Drug Design ◽

Structure Activity Relationship ◽

Activity Relationship ◽

Structure Activity

Download Full-text

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

Thrombosis and Haemostasis ◽

10.1160/th13-08-0635 ◽

2014 ◽

Vol 111 (03) ◽

pp. 429-437 ◽

Cited By ~ 33

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.

Download Full-text