Synthesis and biological evaluation of new cephalosporin derivatives containing cyclic disulfide moieties

Due to a steady increase of microbial resistance, there is a need to increase the effectiveness of antibiotic performance by involving additional mechanisms of their penetration or retention for their better action. Cephalosporins are a successful group of antibiotics to combat pathogenic microorganisms, including drug-resistant strains. In this study, we investigated the effect of newly synthesized cephalosporin derivatives with cyclic disulfide modifications against several Gram-positive and Gram-negative strains as well as against biofilm formation. The incorporation of asparagusic acid was found to be effective in improving the activity of the drug against Gram-negative strains. Furthermore, we could demonstrate the successful inhibition of biofilm formation for S. aureus and P. aeruginosa at similar concentrations as obtained against planktonic cells. We propose that the incorporation of cyclic disulfides is one additional strategy to improve antibiotic activity and to combat bacterial infections.

Synthesis and biological evaluation of novel acyclic and cyclic glyoxamide based derivatives as bacterial quorum sensing and biofilm inhibitors

Organic & Biomolecular Chemistry ◽

10.1039/c7ob01011g ◽

2017 ◽

Vol 15 (27) ◽

pp. 5743-5755 ◽

Cited By ~ 8

Author(s):

Shashidhar Nizalapur ◽

Onder Kimyon ◽

Eugene Yee ◽

Mohan M. Bhadbhade ◽

Mike Manefield ◽

...

Keyword(s):

Quorum Sensing ◽

Biofilm Formation ◽

Biological Evaluation ◽

Gram Negative Bacteria ◽

Gram Negative ◽

E Coli ◽

Sensing Mechanism ◽

Bacterial Quorum Sensing ◽

Bacterial Quorum ◽

Novel acyclic and cyclic glyoxamides that inhibited quorum sensing mechanism and biofilm formation in Gram-negative bacteria such as P. aeruginosa and E. coli.

Synthesis and biological evaluation of novel 4-oxo-5-cyano thiouracil derivatives as SecA inhibitors

Heterocyclic Communications ◽

10.1515/hc-2020-0100 ◽

2020 ◽

Vol 26 (1) ◽

pp. 76-83

Author(s):

Fante Bamba ◽

Jinshan Jin ◽

Phang C. Tai ◽

Binghe Wang

Keyword(s):

Human Health ◽

Biological Evaluation ◽

Drug Resistant ◽

Antimicrobial Evaluation ◽

Resistant Strains ◽

Drug Resistant Strains ◽

Synthesis And Biological Evaluation ◽

Thiouracil Derivatives

AbstractThe continuous emergence of drug-resistant strains of bacteria poses an urgent risk to human health and dictates the need for new antimicrobials. Along this line, we have been working on developing inhibitors of SecA, a key component of the bacterial Sec-dependent secretion machinery. Herein, we describe the synthesis and antimicrobial evaluation of 6-oxo-1,6-dihydropyrimidine-5-carbonitrile derivatives as potential SecA inhibitors.

Halogen-Furan-2(5H)-One Derivatives Decrease Biofilm Production in Pseudomonas aeruginosa.

10.20944/preprints202111.0105.v1 ◽

2021 ◽

Author(s):

Nelly Araceli Aburto-Rodríguez ◽

Rodolfo García-Contreras ◽

Israel Castillo-Juárez ◽

Victor Alberto Castro-Torres ◽

Mariano Martínez-Vázquez

Keyword(s):

Biofilm Formation ◽

Bacterial Infections ◽

Clinical Evidence ◽

Drug Resistant ◽

Swarming Motility ◽

Biofilm Production ◽

Planktonic Form ◽

Severe Infections ◽

Resistant Strains ◽

Clinical evidence has shown that bacterial infections are more difficult to eradicate when form-ing a biofilm aggregate than when are produced by bacteria in planktonic form. Therefore, com-pounds that inhibit biofilm formation could be used against severe infections. It has been re-ported that bromo 2-(5H) furanones inhibited biofilm formation by their anti-quorum sensing properties. To determine if the 2-(5H) furanone moiety is essential to induce inhibition of biofilm formation, we evaluated ten halogen 2-(5H) furanones derivates previously synthesized. Besides evaluating the inhibition of biofilm formation, we assessed pyocyanin production, swarming motility, and transcription of essential QS genes: rsaL, rhlA, pqsA and phz1 genes. Our results showed that although three bromo-furan-2(5H)-one-type derivatives (A1-A3) and two bromo-4-(phenylamino)-furan-2(5H)-one-type compounds (B2 and B6) inhibited the biofilm formation in both P. aeruginosa PA14 (reference) and PA64 (drug-resistant) strains only the furanones A1-A3 were efficient to inhibit QSS.

Design, Synthesis, and Biological Evaluation of Novel Pyrimido[4,5-b]indole Derivatives Against Gram-Negative Multidrug-Resistant Pathogens

Journal of Medicinal Chemistry ◽

10.1021/acs.jmedchem.1c00621 ◽

2021 ◽

Author(s):

Qidi Kong ◽

Wei Pan ◽

Heng Xu ◽

Yaru Xue ◽

Bin Guo ◽

...

Keyword(s):

Multidrug Resistant ◽

Biological Evaluation ◽

Indole Derivatives ◽

Design Synthesis ◽

Gram Negative ◽

Multidrug Resistant Pathogens ◽

ROOM TEMPERATURE SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME 2,5-DISUBSTITUTED-1,3,4-OXADIAZOLES

INDIAN DRUGS ◽

10.53879/id.54.05.10949 ◽

2017 ◽

Vol 54 (05) ◽

pp. 11-15

Author(s):

R. R Somani ◽

◽

P. K Chaskar ◽

P. M. Patil

Keyword(s):

Heterocyclic Compounds ◽

Room Temperature ◽

Antimicrobial Agents ◽

Biological Evaluation ◽

Spectroscopic Techniques ◽

Temperature Synthesis ◽

Room Temperature Synthesis ◽

Synthetic Reactions ◽

Resistant Strains ◽

One of the principles of green chemistry emphasises on minimisation of environmental and economic impacts by developing synthetic reactions at ambient temperature and pressure.The rise of resistant strains of microorganisms is an issue of regularly expanding seriousness. Therefore, the development of new antimicrobial agents will remain a challenge for chemists. we herein report room temperature synthesis of newer heterocyclic compounds belonging to 1,3,4-oxadiazole scaffold. Their structures were confirmed using various spectroscopic techniques. These compounds were evaluated for antifungal, antibacterial and antitubercular activities.

Isolation, Characterization, and Comparison of Efficiencies of Bacteriophages to Reduce Planktonic and Biofilm-Associated Staphylococcus aureus

Journal of Health and Allied Sciences NU ◽

10.1055/s-0040-1715773 ◽

2020 ◽

Vol 10 (03) ◽

pp. 102-108

Author(s):

Anoopkrishna Rai ◽

Rajeshwari V. Vittal ◽

Juliet R. Mohan Raj

Keyword(s):

Staphylococcus Aureus ◽

Biofilm Formation ◽

Bacterial Infections ◽

Viable Cell ◽

Viable Count ◽

Dna Fingerprint ◽

Planktonic Cells ◽

Microtiter Plates ◽

Reduction Assay ◽

Need To Evaluate

Abstract Introduction In the present era, wherein occurrence of antimicrobial resistance compounded with biofilms in disease conditions has rendered present antibiotic therapy ineffective, the need for alternative strategies to treat bacterial infections has brought bacteriophages to the forefront. The antimicrobial activity of phages is often determined by a viable cell reduction assay which focuses only on planktonic forms. The physiology of an organism in biofilm differs from those that are planktonic; hence, there is a need to evaluate the activity of phages both on planktonic forms, as well as on biofilms, to select candidate therapeutic phages. Materials and Methods Bacteriophages for Staphylococcus aureus were isolated from environmental samples and characterized based on growth kinetics and DNA fingerprint patterns. Activity of isolated phages on planktonic forms was determined by viable count reduction assay. Phage ability to prevent biofilm formation and ability to disperse formed biofilms were performed in 96-well microtiter plates and biofilm estimated by crystal violet assay. Results Four bacteriophages designated, that is, P3, PD1, PE1, and PE2, were isolated and characterized. Planktonic cells of S. aureus were found to be sensitive to phages PD1, PE1, and PE2. Phages PD1 and PE2 were efficient in preventing biofilm formation and phages PD1, PE1, and P3 were efficient in dispersing formed biofilms. Conclusion The ability of some phages to disperse biofilms effectively, while unable to show the same efficiency on planktonic cells, indicates that viable count reduction assay alone may not be a sufficient tool to imply bactericidal activity of bacteriophages, especially while trying to eradicate biofilms.

Identification, Typing, Antifungal Resistance Profile, and Biofilm Formation ofCandida albicansIsolates from Lebanese Hospital Patients

BioMed Research International ◽

10.1155/2014/931372 ◽

2014 ◽

Vol 2014 ◽

pp. 1-10 ◽

Cited By ~ 13

Author(s):

Ibrahim Bitar ◽

Roy A. Khalaf ◽

Houda Harastani ◽

Sima Tokajian

Keyword(s):

Biofilm Formation ◽

Fungal Pathogens ◽

Recurrent Infection ◽

Multidrug Resistant ◽

Antifungal Resistance ◽

Drug Resistant ◽

Treatment Regimens ◽

Evolutionary Relatedness ◽

Resistant Strains ◽

As leading opportunistic fungal pathogens identification and subtyping ofCandidaspecies are crucial in recognizing outbreaks of infection, recognizing particularly virulent strains, and detecting the emergence of drug resistant strains. In this study our objective was to compare identification ofCandida albicansby the hospitals through the use of conventional versus identification based on the ITS (Internal Transcribed Spacer) and to assess biofilm forming capabilities, drug resistance patterns and correlate these with MLST typing. ITS typing revealed a 21.2% hospital misidentification rate. Multidrug resistance to three drugs out of four tested was detected within 25% of the isolates raising concerns about the followed treatment regimens. Drug resistant strains as well as biofilm formers were phylogenetically related, with some isolates with significant biofilm forming capabilities being correlated to those that were multidrug resistant. Such isolates were grouped closely together in a neighbor-joining tree generated by MLST typing indicating phylogenetic relatedness, microevolution, or recurrent infection. In conclusion, this pilot study gives much needed insight concerningC. albicansisolates circulating in Lebanese hospitals and is the first study of its kind correlating biofilm formation, antifungal resistance, and evolutionary relatedness.

Biological Evaluation of Potent Triclosan-Derived Inhibitors of the Enoyl-Acyl Carrier Protein Reductase InhA in Drug-Sensitive and Drug-Resistant Strains ofMycobacterium tuberculosis

ChemMedChem ◽

10.1002/cmdc.201402255 ◽

2014 ◽

Vol 9 (11) ◽

pp. 2528-2537 ◽

Cited By ~ 18

Author(s):

Jozef Stec ◽

Catherine Vilchèze ◽

Shichun Lun ◽

Alexander L. Perryman ◽

Xin Wang ◽

...

Keyword(s):

Acyl Carrier Protein ◽

Biological Evaluation ◽

Carrier Protein ◽

Drug Resistant ◽

Ofmycobacterium Tuberculosis ◽

Resistant Strains ◽

Synthesis and biological evaluation of new Benzimidazole derivatives

Al-Mustansiriyah Journal of Science ◽

10.23851/mjs.v29i1.127 ◽

2018 ◽

Vol 29 (1) ◽

pp. 107 ◽

Cited By ~ 2

Author(s):

Hadeel Majed ◽

Firyal W. Askar

Keyword(s):

Schiff Bases ◽

Nmr Spectra ◽

Antimicrobial Activities ◽

Biological Evaluation ◽

Benzimidazole Derivatives ◽

Gram Negative Bacteria ◽

Gram Negative ◽

H Nmr ◽

Bacteria And Fungi ◽

Agroup of benzimidazole derivatives bearing different heterocyclic moieties such as Schiff bases, 2-azetidinone and 4-thiazolidinone were efficiently prepared. The structures of the newly compounds were characterized by FTIRand ¹H NMR spectra. The synthesized compounds were evaluated for their antimicrobial activities against gram-positive and gram negative bacteria and fungi using the microdilution procedure.

Antimicrobial Activity of Extracts of Two Native Fruits of Chile: Arrayan (Luma apiculata) and Peumo (Cryptocarya alba)

Antibiotics ◽

10.3390/antibiotics9080444 ◽

2020 ◽

Vol 9 (8) ◽

pp. 444

Author(s):

Jitka Viktorová ◽

Rohitesh Kumar ◽

Kateřina Řehořová ◽

Lan Hoang ◽

Tomas Ruml ◽

...

Keyword(s):

Mass Spectrometry ◽

Inhibitory Concentration ◽

Dependent Manner ◽

Drug Resistant ◽

Planktonic Cells ◽

Fruit Extract ◽

Concentration Dependent Manner ◽

Autoinducer 2 ◽

Resistant Strains ◽

Arrayan and peumo fruits are commonly used in the traditional medicine of Chile. In this study, the concentration of the extracts halving the bacterial viability and biofilms formation and disruption of the drug-sensitive and drug-resistant strains of Staphylococcus aureus and Pseudomonas aeruginosa was determined. The chemical composition of extracts was analyzed by high-resolution liquid chromatography coupled with mass spectrometry (U-HPLC/MS). The arrayan extract (Inhibitory concentration IC50 0.35 ± 0.01 mg/mL) was more effective than peumo extract (IC50 0.53 ± 0.02 mg/mL) in the inhibition of S. aureus planktonic cells. Similarly, the arrayan extract was more effective in inhibiting the adhesion (S. aureus IC50 0.23 ± 0.02 mg/mL, P. aeruginosa IC50 0.29 ± 0.02 mg/mL) than peumo extracts (S. aureus IC50 0.47 ± 0.03 mg/mL, P. aeruginosa IC50 0.35 ± 0.01 mg/mL). Both extracts inhibited quorum sensing in a concentration-dependent manner, and the most significant was the autoinducer-2 type communication inhibition by arrayan extract. Both extracts also disrupted preformed biofilm of P. aeruginosa (arrayan IC50 0.56 ± 0.04 mg/mL, peumo IC50 0.59 ± 0.04 mg/mL). However, neither arrayan nor peumo extracts disrupted S. aureus mature biofilm. U-HPLC/MS showed that both fruit extracts mainly possessed quercetin compounds; the peumo fruit extract also contained phenolic acids and phenylpropanoids. Our results suggested that both extracts could be used as natural antimicrobials for some skin and nosocomial infections.