Synthesis, antibacterial and antifungal activities of naphthoquinone derivatives: a structure–activity relationship study

2016 ◽  
Vol 25 (6) ◽  
pp. 1274-1285 ◽  
Author(s):  
Juan M. Sánchez-Calvo ◽  
Gara R. Barbero ◽  
Guillermo Guerrero-Vásquez ◽  
Alexandra G. Durán ◽  
Mariola Macías ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Structure Activity ◽  
Relationship Study ◽  
Antibacterial And Antifungal

scholarly journals Guanidine-Containing Polyhydroxyl Macrolides: Chemistry, Biology, and Structure-Activity Relationship

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3913 ◽  
Author(s):  
Xiaoyuan Song ◽  
Ganjun Yuan ◽  
Peibo Li ◽  
Sheng Cao
Keyword(s):  
Antimicrobial Agents ◽  
Lactone Ring ◽  
Lipoteichoic Acid ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Side Chain ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Structure Activity ◽  
Antibacterial And Antifungal

Antimicrobial resistance has been seriously threatening human health, and discovering new antimicrobial agents from the natural resource is still an important pathway among various strategies to prevent resistance. Guanidine-containing polyhydroxyl macrolides, containing a polyhydroxyl lactone ring and a guanidyl side chain, can be produced by many actinomycetes and have been proved to possess many bioactivities, especially broad-spectrum antibacterial and antifungal activities. To explore the potential of these compounds to be developed into new antimicrobial agents, a review on their structural diversities, spectroscopic characterizations, bioactivities, acute toxicities, antimicrobial mechanisms, and the structure-activity relationship was first performed based on the summaries and analyses of related publications from 1959 to 2019. A total of 63 guanidine-containing polyhydroxyl macrolides were reported, including 46 prototype compounds isolated from 33 marine and terrestrial actinomycetes and 17 structural derivatives. Combining with their antimicrobial mechanisms, structure-activity relationship analyses indicated that the terminal guanidine group and lactone ring of these compounds are vital for their antibacterial and antifungal activities. Further, based on their bioactivities and toxicity analyses, the discovery of guanidyl side-chain targeting to lipoteichoic acid of Staphylococcus aureus indicated that these compounds have a great potency to be developed into antimicrobial and anti-inflammatory drugs.

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.

Strategic structure-activity relationship study on a follistatin-derived myostatin inhibitory peptide

2021 ◽  
pp. 128163
Author(s):  
Mariko Saitoh ◽  
Kentaro Takayama ◽  
Yoshimi Roppongi ◽  
Takahiro Shimada ◽  
Akihiro Taguchi ◽  
...  
Keyword(s):  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Inhibitory Peptide ◽  
Structure Activity ◽  
Relationship Study

Structure-activity relationship study of vitamin D analogs with oxolane group in their side chain

2017 ◽  
Vol 134 ◽  
pp. 86-96 ◽  
Author(s):  
Anna Y. Belorusova ◽  
Andrea Martínez ◽  
Zoila Gándara ◽  
Generosa Gómez ◽  
Yagamare Fall ◽  
...  
Keyword(s):  
Vitamin D ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Side Chain ◽  
Vitamin D Analogs ◽  
Structure Activity ◽  
Relationship Study
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