Antioxidant and Antibacterial Activity of Sulfonamides Derived from Carvacrol: A Structure-Activity Relationship Study

2020 ◽  
Vol 20 (3) ◽  
pp. 173-181 ◽  
Author(s):  
Aldo S. de Oliveira ◽  
Luiz F. S. de Souza ◽  
Ricardo J. Nunes ◽  
Susana Johann ◽  
David L. Palomino-Salcedo ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Biological Activity ◽  
Molecular Docking ◽  
Small Molecule ◽  
Bacterial Resistance ◽  
Mechanisms Of Action ◽  
New Drugs ◽  
Structure Activity ◽  
Relationship Study ◽  
Antibacterial Potential

Background: Bacterial resistance to antibiotics is a growing problem in all countries and has been discussed worldwide. In this sense, the development of new drugs with antibiotic properties is highly desirable in the context of medicinal chemistry. Methodology: In this paper we investigate the antioxidant and antibacterial potential of sulfonamides derived from carvacrol, a small molecule with drug-like properties. Most sulfonamides had antioxidant and antibacterial potential, especially compound S-6, derived from beta-naphthylamine. Result: To understand the possible mechanisms of action involved in biological activity, the experimental results were compared with molecular docking data. Conclusion: This research allows appropriate discussion on the identified structure activity relationships.

Biological Activity of Trans-Membrane Anion Carriers

2018 ◽  
Vol 25 (30) ◽  
pp. 3560-3576 ◽  
Author(s):  
Massimo Tosolini ◽  
Paolo Pengo ◽  
Paolo Tecilla
Keyword(s):  
Biological Activity ◽  
Membrane Transport ◽  
Anticancer Agents ◽  
Biological Effects ◽  
Structure Activity Relationship ◽  
New Drugs ◽  
Activity Relationship ◽  
Anion Channels ◽  
Cellular Homeostasis ◽  
Structure Activity

Natural and synthetic anionophores promote the trans-membrane transport of anions such as chloride and bicarbonate. This process may alter cellular homeostasis with possible effects on internal ions concentration and pH levels triggering several and diverse biological effects. In this article, an overview of the recent results on the study of aniontransporters, mainly acting with a carrier-type mechanism, is given with emphasis on the structure/activity relationship and on their biological activity as antibiotic and anticancer agents and in the development of new drugs for treating conditions derived from dysregulation of natural anion channels.

Review: Studies on the Synthesis of Quinolone Derivatives with Their Antibacterial Activity (Part 1)

2020 ◽  
Vol 24 (8) ◽  
pp. 817-854
Author(s):  
Anil Kumar ◽  
Nishtha Saxena ◽  
Arti Mehrotra ◽  
Nivedita Srivastava
Keyword(s):  
Antibacterial Activity ◽  
Antibacterial Properties ◽  
Structure Activity Relationship ◽  
New Drugs ◽  
Activity Relationship ◽  
Structure Activity ◽  
Medicinal Properties ◽  
Synthetic Routes ◽  
Quinolone Derivatives

Quinolone derivatives have attracted considerable attention due to their medicinal properties. This review covers many synthetic routes of quinolones preparation with their antibacterial properties. Detailed study with structure-activity relationship among quinolone derivatives will be helpful in designing new drugs in this field.

scholarly journals New Mononuclear and Binuclear Cu(II), Co(II), Ni(II), and Zn(II) Thiosemicarbazone Complexes with Potential Biological Activity: Antimicrobial and Molecular Docking Study

Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2288
Author(s):  
Ahmed Gaber ◽  
Moamen S. Refat ◽  
Arafa A.M. Belal ◽  
Ibrahim M. El-Deen ◽  
Nader Hassan ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Biological Activity ◽  
Molecular Docking ◽  
Metal Complexes ◽  
Analytical Data ◽  
Docking Study ◽  
Spectroscopic Techniques ◽  
Molecular Docking Study ◽  
Tetrahedral Geometry ◽  
Thiosemicarbazone Complexes

Herein, we report the synthesis of eight new mononuclear and binuclear Co2+, Ni2+, Cu2+, and Zn2+ methoxy thiosemicarbazone (MTSC) complexes aiming at obtaining thiosemicarbazone complex with potent biological activity. The structure of the MTSC ligand and its metal complexes was fully characterized by elemental analysis, spectroscopic techniques (NMR, FTIR, UV-Vis), molar conductivity, thermogravimetric analysis (TG), and thermal differential analysis (DrTGA). The spectral and analytical data revealed that the obtained thiosemicarbazone-metal complexes have octahedral geometry around the metal center, except for the Zn2+-thiosemicarbazone complexes, which showed a tetrahedral geometry. The antibacterial and antifungal activities of the MTSC ligand and its (Co2+, Ni2+, Cu2+, and Zn2+) metal complexes were also investigated. Interestingly, the antibacterial activity of MTSC- metal complexes against examined bacteria was higher than that of the MTSC alone, which indicates that metal complexation improved the antibacterial activity of the parent ligand. Among different metal complexes, the MTSC- mono- and binuclear Cu2+ complexes showed significant antibacterial activity against Bacillus subtilis and Proteus vulgaris, better than that of the standard gentamycin drug. The in silico molecular docking study has revealed that the MTSC ligand could be a potential inhibitor for the oxidoreductase protein.

scholarly journals ANTIBACTERIAL ACTIVITY OF THE ETHANOL EXTRACT OF Eugenia dysenterica DC (MYRTACEAE)

2019 ◽  
Vol 16 (32) ◽  
pp. 257-262
Author(s):  
Thaís Paula Rodrigues GONÇALVES ◽  
William Gustavo LIMA ◽  
Izabela Caputo Assis SILVA ◽  
Adriano Guimarães PARREIRA ◽  
Luciana Alves Rodrigues dos Santos LIMA
Keyword(s):  
Bacterial Resistance ◽  
Ethanol Extract ◽  
New Drugs ◽  
Bactericidal Action ◽  
Phytochemical Screening ◽  
Biological Potential ◽  
Important Field ◽  
Phytochemical Profile ◽  
Eugenia Dysenterica ◽  
Antibacterial Potential

The large variety of plant specimens found in Brazil with still unexplored medicinal potential, combined with the increase in bacterial resistance to antimicrobials traditionally employed, opens an important field of research aimed at prospecting new drugs. In this context the objective of this work was to evaluate the antibacterial potential of Eugenia dysenterica and to characterize its phytochemical profile. Ethanolic extracts were obtained by drying, grinding, turbo-extraction and lyophilization of the leaves of the plant. The CIM and CBM tests were performed to evaluate the antimicrobial potential on the following strains: Proteus mirabilis ATCC 15290, Echerichia coli ATCC25922, Staphylococcus aureus ATCC29213 and Staphylococcus epidermides ATCC 12228. E. dysenterica presented bactericidal action at 2mg.ml-1 against S. aureus and bacteriostatic at 1mg.ml-1 against P. mirabilis. Several phenolic compounds were detected in the phytochemical screening, and the presence of these compounds may justify the biological potential of this plant.

scholarly journals Aromatic Hydroxyl Group Plays a Critical Role in Antibacterial Activity of the Curcumin Analogues

2012 ◽  
Vol 7 (1) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Mi Kyoung Kim ◽  
Jun Cheol Park ◽  
Youhoon Chong
Keyword(s):  
Antibacterial Activity ◽  
Critical Role ◽  
Antibacterial Activities ◽  
Structure Activity Relationship ◽  
Activity Relationship ◽  
Hydroxyl Group ◽  
Curcumin Analogues ◽  
Structure Activity ◽  
Relationship Study

The aim of this study was to investigate the role of the aromatic substituents of the curcumin scaffold on the antibacterial activity of the resulting curcumin analogues. Six curcumin analogues with different aromatic substituents were prepared and their antibacterial activities were evaluated against two Gram-positive and four Gram-negative bacteria. The structure-activity relationship study demonstrated that antibacterial activity of the curcumin analogues was critically dependent upon the aromatic hydroxyl group. Thus, hydroxycurcumin with an additional aromatic hydroxyl group on the curcumin scaffold showed antibacterial activity against all six pathogens tested and it remained effective even against ampicillin-resistant Enterobacter cloacae. Along with the previously reported antioxidative effect, the broad-spectrum antibacterial activity of the hydroxycurcumin warrants further investigation of its biological activity as well as extensive structure-activity relationship study of the curcumin analogues with various aromatic substituents.

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