scholarly journals Structure-Activity Relationships of the Imidazolium Compounds as Antibacterials of Staphylococcus aureus and Pseudomonas aeruginosa

2021 ◽  
Vol 22 (15) ◽  
pp. 7997
Author(s):  
Łukasz Pałkowski ◽  
Maciej Karolak ◽  
Jerzy Błaszczyński ◽  
Jerzy Krysiński ◽  
Roman Słowiński
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Surface Properties ◽  
Decision Rules ◽  
Rank Condition ◽  
Confirmation Measure ◽  
Sar Studies ◽  
Structure Activity ◽  
Decision Attributes ◽  
Sar Analysis

This paper presents the results of structure–activity relationship (SAR) studies of 140 3,3’-(α,ω-dioxaalkan)bis(1-alkylimidazolium) chlorides. In the SAR analysis, the dominance-based rough set approach (DRSA) was used. For analyzed compounds, minimum inhibitory concentration (MIC) against strains of Staphylococcus aureus and Pseudomonas aeruginosa was determined. In order to perform the SAR analysis, a tabular information system was formed, in which tested compounds were described by means of condition attributes, characterizing the structure (substructure parameters and molecular descriptors) and their surface properties, and a decision attribute, classifying compounds with respect to values of MIC. DRSA allows to induce decision rules from data describing the compounds in terms of condition and decision attributes, and to rank condition attributes with respect to relevance using a Bayesian confirmation measure. Decision rules present the most important relationships between structure and surface properties of the compounds on one hand, and their antibacterial activity on the other hand. They also indicate directions of synthesizing more efficient antibacterial compounds. Moreover, the analysis showed differences in the application of various parameters for Gram-positive and Gram-negative strains, respectively.

Characterization of electrical surface properties of mono- and co-cultures of Pseudomonas aeruginosa and methicillin-resistant Staphylococcus aureus using Kelvin probe force microscopy

RSC Advances ◽  
2014 ◽  
Vol 4 (80) ◽  
pp. 42432-42440 ◽  
Author(s):  
Eric Birkenhauer ◽  
Suresh Neethirajan
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Surface Properties ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Kelvin Probe Force Microscopy ◽  
Bacterial Cells ◽  
Kelvin Probe ◽  
Potential Measurement ◽  
Force Microscopy

Quantitative nanoscale surface potential measurement of individual pathogenic bacterial cells for understanding the adhesion kinetics using Kelvin probe force microscopy.

Synthesis and SAR Study of Simple Aryl Oximes and Nitrofuranyl Derivatives with Potent Activity Against Mycobacterium tuberculosis

2019 ◽  
Vol 17 (1) ◽  
pp. 12-20
Author(s):  
Cristiane França da Costa ◽  
Marcus Vinicius Nora de Souza ◽  
Maria Cristina da Silva Lourenço ◽  
Elaine Soares Coimbra ◽  
Guilherme da Silva Lourenço Carvalho ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Mycobacterium Tuberculosis ◽  
Rational Design ◽  
Biological Activities ◽  
Shigella Flexneri ◽  
Selectivity Index ◽  
Mycobacterium Tuberculosis H37rv ◽  
Structure Activity ◽  
Sar Study

Background: Oximes and nitrofuranyl derivatives are particularly important compounds in medicinal chemistry. Thus, many researchers have been reported to possess antibacterial, antiparasitic, insecticidal and fungicidal activities. Methods: In this work, we report the synthesis and the biological activity against Mycobacterium tuberculosis H37RV of a series of fifty aryl oximes, ArCH=N-OH, I, and eight nitrofuranyl compounds, 2-nitrofuranyl-X, II. Results: Among the oximes, I: Ar = 2-OH-4-OH, 42, and I: Ar = 5-nitrofuranyl, 46, possessed the best activity at 3.74 and 32.0 µM, respectively. Also, 46, the nitrofuran compounds, II; X = MeO, 55, and II: X = NHCH2Ph, 58, (14.6 and 12.6 µM, respectively), exhibited excellent biological activities and were non-cytotoxic. Conclusion: The compound 55 showed a selectivity index of 9.85. Further antibacterial tests were performed with compound 55 which was inactive against Enterococcus faecalis, Klebisiella pneumonae, Pseudomonas aeruginosa, Staphylococcus aureus, Salmonella typhymurium and Shigella flexneri. This study adds important information to the rational design of new lead anti-TB drugs. Structure-activity Relationship (SAR) is reported.

scholarly journals Synthesis and Evaluation of Some New Thiazolidin-4-One Derivatives as Potential Antimicrobial Agents

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
B. A. Baviskar ◽  
S. S. Khadabadi ◽  
S. L. Deore
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antimicrobial Agents ◽  
Salmonella Typhi ◽  
Zone Of Inhibition ◽  
Structure Activity

A new series ofN-{4-methyl-5-[4-(4-oxo-2-phenyl(1,3-thiazolidin-3-yl)]-5-sulfanyl(1,2,4-triazol-3-yl)-1,3-thiazol-2-yl }acetamide (7a-l) was synthesized in order to determine their antimicrobial activity and feasible structure–activity relationships. The compounds were synthesized in good yield and the structures of all newly synthesized compounds were established on the basis of their IR,1HNMR, and elemental analysis. The synthesized compounds were testedin vitroantibacterial activity againstStaphylococcus aureus,Escherichia coli,Pseudomonas aeruginosaandSalmonella typhiand antifungal activity againstAspergillus niger,Candida albicansby measuring the zone of inhibition in mm.

Access to a Library of 1,3-disubstituted-1,2,3-triazenes and Evaluation of their Antimicrobial Properties

2020 ◽  
Vol 20 (9) ◽  
pp. 713-719 ◽  
Author(s):  
Insa Seck ◽  
Samba F. Ndoye ◽  
Lalla A. Ba ◽  
Alioune Fall ◽  
Abdoulaye Diop ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Candida Albicans ◽  
Enterococcus Faecalis ◽  
Therapeutic Potential ◽  
Rapid Development ◽  
Antimicrobial Properties ◽  
Structure Activity

Background: Due to the rapid development of microbial resistance, finding new molecules became urgent to counteract this problem. Objective: The objective of this work is to access 1,2,3-triazene-1,3-disubstituted, a class of molecule with high therapeutic potential. Methods: Here we describe the access to 17 new triazene including six with an imidazole-1,2,3-triazene moiety and eleven with an alkyl-1,2,3-triazene moiety and their evaluation against five strains: two gram (-): Escherichia coli ATCC 25921 and Pseudomonas aeruginosa ATCC 27253; two gram (+) : Staphylococcus aureus ATCC 38213 and Enterococcus faecalis ATCC 29212; and one fungi: Candida albicans ATCC 24433. Results: All strains were sensitive and the best MIC, 0.28 µM, is observed for 4c against Escherichia coli ATCC 25921. Compound 9, 3-isopropynyltriazene, appears to be the most interesting since it is active on the five evaluated strains with satisfactory MIC 0.32 µM against Escherichia coli and Pseudomonas aeruginosa and 0.64 µM against Enterococcus faecalis and Pseudomonas aeruginosa. Conclusion: Comparing the structure activity relationship, electron withdrawing groups appear to increase antimicrobial activity.

Case of a diabetic man cured from rhinocerebral zygomycosis

2010 ◽  
Vol 151 (39) ◽  
pp. 1591-1596
Author(s):  
Botond Lakatos ◽  
Radka Nikolova ◽  
László Ocskay ◽  
Judit Csomor ◽  
Gyula Prinz
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Amphotericin B ◽  
Rhizopus Oryzae

A zygomycosis (mucormycosis) ritka, kifejezetten agresszív lefolyású opportunista infekció, amelyet a Zygomycota (Járomspórás gombák) törzs Zygomycetes osztályába tartozó gombák okoznak. Jellemzően immunhiány, neutropenia, vastúlterhelés, hematológiai betegség, illetve diabeteses ketoacidosis eseteiben fordul elő. Esetismertetés: A szerzők 18 éves, 9 éve inzulindependens diabetes mellitusban szenvedő, rossz compliance-szel rendelkező beteg kórtörténetét ismertetik. Súlyos állapotban, beszűkült tudattal, ketoacidosisban, orrmelléküreg-gyulladásra utaló egyoldali periorbitalis duzzanattal, bőrpírral került kórházba. Bár az endoszkópos sinusműtét során vett váladékból methicillinrezisztens Staphylococcus aureus és Pseudomonas aeruginosa tenyészett, a beteg anamnézise, klinikuma zygomycosis gyanúját keltette, emiatt amphotericin-B-kezelést indítottak. Szövettani, illetve mikrobiológiai vizsgálatok során Rhizopus oryzae okozta invazív infekció igazolódott. Megbeszélés: Az antifungális kezelés ismételt sebészeti beavatkozásokkal és adjuváns granulocytakolónia-stimuláló faktor alkalmazásával kiegészítve eredményesnek bizonyult. A beteg négy hónappal hazabocsátását követően él és panaszmentes. Orv. Hetil., 2010, 39, 1591–1596.

Antibacterial Activity of Desert Truffles from Saudi Arabia Against Staphylococcus aureus and Pseudomonas aeruginosa

2017 ◽  
Vol 19 (2) ◽  
pp. 121-125 ◽  
Author(s):  
Domenico Schillaci ◽  
Maria Grazia Cusimano ◽  
Stella Maria Cascioferro ◽  
Vita Di Stefano ◽  
Vincenzo Arizza ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antibacterial Activity ◽  
Saudi Arabia ◽  
Desert Truffles

The Study of Bacillus Subtils Antimicrobial Activity on Some of the Pathological Isolates

2019 ◽  
Vol 9 (02) ◽  
Author(s):  
Hussein A Kadhum ◽  
Thualfakar H Hasan2
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Bacillus Subtilis ◽  
Bacterial Growth ◽  
Broad Spectrum ◽  
Inhibitory Activity ◽  
Bacterial Pathogens ◽  
Inhibitory Ability ◽  
Selection Of

The study involved the selection of two isolates from Bacillus subtilis to investigate their inhibitory activity against some bacterial pathogens. B sub-bacteria were found to have a broad spectrum against test bacteria such as Staphylococcus aureus and Pseudomonas aeruginosa. They were about 23-30 mm and less against Klebsiella sp. The sensitivity of some antibodies was tested on the test samples. The results showed that the inhibitory ability of bacterial growth in the test samples using B. subtilis extract was more effective than the antibiotics used.

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