scholarly journals (+)-epi-Epoformin, a Phytotoxic Fungal Cyclohexenepoxide: Structure Activity Relationships

2018 ◽  
Author(s):  
Antonio Cala ◽  
Marco Masi ◽  
Alessio Cimmino ◽  
José M.G. Molinillo ◽  
Francisco A. Macías ◽  
...  
Keyword(s):  
Fungal Pathogen ◽  
Biological Activities ◽  
Spectroscopic Characterization ◽  
Structure Activity Relationship ◽  
Significant Loss ◽  
Cork Oak ◽  
Activity Relationship ◽  
Wheat Coleoptile ◽  
Phytotoxic Activity ◽  
Structure Activity

(+)-epi-Epoformin (1), is a fungal cyclohexene epoxide isolated together with diplopimarane and sphaeropsidins A and C, a nor-ent-pimarane and two pimaranes, from the culture filtrates of Diplodia quercivora, a fungal pathogen for cork oak in Sardinia, Italy. Compound 1 possesses a plethora of biological activities including: antifungal, zootoxic and phytotoxic activity. The last activity and the peculiar structural feature of 1 suggested to carry out a structure activity relationship study, preparing eight key hemisynthetic derivatives and their phytotoxicity was assayed. The complete spectroscopic characterization and the activity in the etiolated wheat coleoptile bioassay of all the compounds is reported. Most of the compounds inhibited growth and some of them had comparable or higher activity than the natural product and the reference herbicide Logran. As regards the structure-activity relationship, the carbonyl proved to be essential for their activity of 1, as well as the conjugated double bond, while the epoxide could be altered with no significant loss.

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 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.

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.

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

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.

scholarly journals Sense Ginsenosides From Ginsengs: Structure-Activity Relationship in Autophagy

2019 ◽  
Vol 14 (6) ◽  
pp. 1934578X1985822
Author(s):  
Tao Wu ◽  
Osafo Raymond Kwaku ◽  
Hai-Zhou Li ◽  
Chong-Ren Yang ◽  
Long-Jiao Ge ◽  
...  
Keyword(s):  
Biological Activities ◽  
Herbal Medicines ◽  
Structural Diversity ◽  
Panax Notoginseng ◽  
American Ginseng ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Clinical Use ◽  
Structure Activity ◽  
Autophagic Activity

The term ginseng refers to the dried roots of several plants belonging to the genus Panax of the Araliaceae family. The 3 major commercial ginsengs are Panax notoginseng (Burk.) F.H. Chen (Notoginseng), P. ginseng C.A. Meyer (Ginseng), and P. quinquefolius L. (American ginseng), which have been used as herbal medicines. Over 18,000 papers on ginsengs have been published on the basis of their structural diversity and biological activities. Many reviews have summarized the phytochemistry, pharmacology, and clinical use of ginsengs, but the structure-activity relationship (SAR) of ginsenosides from ginsengs in autophagy is unavailable. Herein, we review the structural diversity of ginsenosides, especially the ones in notoginseng, and the SAR in autophagic activity is discussed in detail.

scholarly journals Recent Advances in the Semisynthesis, Modifications and Biological Activities of Ocotillol-Type Triterpenoids

Molecules ◽  
2020 ◽  
Vol 25 (23) ◽  
pp. 5562
Author(s):  
Yucheng Cao ◽  
Kaiyi Wang ◽  
Si Xu ◽  
Lingtan Kong ◽  
Yi Bi ◽  
...  
Keyword(s):  
Biological Activities ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Pharmacological Activities ◽  
Structure Activity ◽  
Recent Advances ◽  
The World ◽  
Anti Inflammatory ◽  
Active Substances

Ginseng is one of the most widely consumed herbs in the world and plays an important role in counteracting fatigue and alleviating stress. The main active substances of ginseng are its ginsenosides. Ocotillol-type triterpenoid is a remarkably effective ginsenoside from Vietnamese ginseng that has received attention because of its potential antibacterial, anticancer and anti-inflammatory properties, among others. The semisynthesis, modification and biological activities of ocotillol-type compounds have been extensively studied in recent years. The aim of this review is to summarize semisynthesis, modification and pharmacological activities of ocotillol-type compounds. The structure–activity relationship studies of these compounds were reported. This summary should prove useful information for drug exploration of ocotillol-type derivatives.

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