ChemInform Abstract: Bicyclic Pyrazolidinones, a New Class of Antibacterial Agent Based on the β-Lactam Model. Bicyclic Pyrazolidinones, Steric and Electronic Effects on Antibacterial Activity.

The antibacterial activity of three Cupressaceae plants (Thujaoccidentalis,ThujaorientalisandChamaecyparisobtusa) was tested against three bacteria using the agar diffusion method. The ether and ethylacetate fraction of crude methanol extract from the three plants showed potent antibacterial activity against the tested microorganisms. The result showed that Staphylococcus aureus revealed the most sensitivity among the tested bacteria. Thujaoccidentalisether fraction and Thujaorientalis hexane fraction exhibited the highest antibacterial activity against Staphylococcus aureus. E. coli was shown the highest MIC values compared to the other two tested bacteria, which indicates the lowest antibacterial activity against the bacterium. This study promises an interesting future for designing a potentially active antibacterial agent from the three Cupressaceae plants.

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Large-scale High-throughput Screening Revealed 5'-(carbonylamino)-2,3'- bithiophene-4'-carboxylate as Novel Template for Antibacterial Agents

Current Drug Discovery Technologies ◽

10.2174/1570163816666190603095521 ◽

2020 ◽

Vol 17 (5) ◽

pp. 716-724

Author(s):

Yan A. Ivanenkov ◽

Renat S. Yamidanov ◽

Ilya A. Osterman ◽

Petr V. Sergiev ◽

Vladimir A. Aladinskiy ◽

...

Keyword(s):

Antibacterial Activity ◽

High Throughput ◽

High Throughput Screening ◽

Large Scale ◽

Antibacterial Agents ◽

Sos Response ◽

Luciferase Assay ◽

Translational Machinery ◽

E Coli ◽

New Class

Background: The key issue in the development of novel antimicrobials is a rapid expansion of new bacterial strains resistant to current antibiotics. Indeed, World Health Organization has reported that bacteria commonly causing infections in hospitals and in the community, e.g. E. Coli, K. pneumoniae and S. aureus, have high resistance vs the last generations of cephalosporins, carbapenems and fluoroquinolones. During the past decades, only few successful efforts to develop and launch new antibacterial medications have been performed. This study aims to identify new class of antibacterial agents using novel high-throughput screening technique. Methods: We have designed library containing 125K compounds not similar in structure (Tanimoto coeff.< 0.7) to that published previously as antibiotics. The HTS platform based on double reporter system pDualrep2 was used to distinguish between molecules able to block translational machinery or induce SOS-response in a model E. coli system. MICs for most active chemicals in LB and M9 medium were determined using broth microdilution assay. Results: In an attempt to discover novel classes of antibacterials, we performed HTS of a large-scale small molecule library using our unique screening platform. This approach permitted us to quickly and robustly evaluate a lot of compounds as well as to determine the mechanism of action in the case of compounds being either translational machinery inhibitors or DNA-damaging agents/replication blockers. HTS has resulted in several new structural classes of molecules exhibiting an attractive antibacterial activity. Herein, we report as promising antibacterials. Two most active compounds from this series showed MIC value of 1.2 (5) and 1.8 μg/mL (6) and good selectivity index. Compound 6 caused RFP induction and low SOS response. In vitro luciferase assay has revealed that it is able to slightly inhibit protein biosynthesis. Compound 5 was tested on several archival strains and exhibited slight activity against gram-negative bacteria and outstanding activity against S. aureus. The key structural requirements for antibacterial potency were also explored. We found, that the unsubstituted carboxylic group is crucial for antibacterial activity as well as the presence of bulky hydrophobic substituents at phenyl fragment. Conclusion: The obtained results provide a solid background for further characterization of the 5'- (carbonylamino)-2,3'-bithiophene-4'-carboxylate derivatives discussed herein as new class of antibacterials and their optimization campaign.

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Recent Advances in 1,3,5-Triazine Derivatives as Antibacterial Agents

Mini-Reviews in Organic Chemistry ◽

10.2174/1570193x17666200129094032 ◽

2020 ◽

Vol 17 (8) ◽

pp. 991-1041

Author(s):

Divya Utreja ◽

Jagdish Kaur ◽

Komalpreet Kaur ◽

Palak Jain

Keyword(s):

Antibacterial Activity ◽

Heterocyclic Compounds ◽

Antibacterial Agents ◽

Rapid Development ◽

Pharmacological Action ◽

Biological Properties ◽

Vast Array ◽

Bacterial Diseases ◽

New Class ◽

Triazine Derivatives

Triazine, one of the nitrogen containing heterocyclic compounds has attracted the considerable interest of researchers due to the vast array of biological properties such as anti-viral, antitumor, anti-convulsant, analgesic, antioxidant, anti-depressant, herbicidal, insecticidal, fungicidal, antibacterial and anti-inflammatory activities offered by it. Various antibacterial agents have been synthesized by researchers to curb bacterial diseases but due to rapid development in drug resistance, tolerance and side effects, there had always been a need for the synthesis of a new class of antibacterial agents that would exhibit improved pharmacological action. Therefore, this review mainly focuses on the various methods for the synthesis of triazine derivatives and their antibacterial activity.

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The Preparation of Carbon Microspheres Loading Silver Antimicrobial Agent and the Study of its Properties

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.550-553.1026 ◽

2012 ◽

Vol 550-553 ◽

pp. 1026-1029

Author(s):

Jian Xi Ren ◽

Jing Ya Li ◽

Zhi Feng Cai ◽

Jin Ming Dai ◽

Mei Niu ◽

...

Keyword(s):

Escherichia Coli ◽

Staphylococcus Aureus ◽

Antibacterial Activity ◽

Electron Microscope ◽

Antibacterial Agent ◽

Chemical Adsorption ◽

Carbon Microspheres ◽

Bacterial Inhibition ◽

Good Antibacterial Activity ◽

Scanning Electron

Carbon microspheres (CMSs) were used as the carrier to prepare the Ag-loading CMSs (Ag/CMSs) antibacterial agent through the method of chemical adsorption. The morphologies and structures of modified CMSs were characterized by using the field emission Scanning Electron Microscope (SEM). The results showed that silver was absorbed on the surface of CMSs. The bacterial inhibition ring experiment showed that Ag/CMSs had good antibacterial activity against Staphylococcus aureus and Escherichia coli, meanwhile the diameters of the bacterial inhibition rings were 19 mm against Staphylococcus aureus and 21 mm against Escherichia coli, respectively.

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Construction of a New Class of Tetracycline Lead Structures with Potent Antibacterial Activity through Biosynthetic Engineering

Angewandte Chemie ◽

10.1002/ange.201411028 ◽

2015 ◽

Vol 127 (13) ◽

pp. 4009-4012 ◽

Cited By ~ 1

Author(s):

Urška Lešnik ◽

Tadeja Lukežič ◽

Ajda Podgoršek ◽

Jaka Horvat ◽

Tomaž Polak ◽

...

Keyword(s):

Antibacterial Activity ◽

New Class ◽

Biosynthetic Engineering

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Synthesis and antibacterial activity evaluation of C-5 side chain modified analogues of FYL-66, a potential agent against methicillin-resistant Staphylococcus aureus

MedChemComm ◽

10.1039/c5md00101c ◽

2015 ◽

Vol 6 (6) ◽

pp. 1156-1172 ◽

Cited By ~ 3

Author(s):

Xiaoyan Yang ◽

Zicheng Li ◽

Zhenling Wang ◽

Zitai Sang ◽

Haiyue Long ◽

...

Keyword(s):

Staphylococcus Aureus ◽

Antibacterial Activity ◽

Animal Models ◽

Antibacterial Agent ◽

Methicillin Resistant Staphylococcus Aureus ◽

Biological Activities ◽

Side Chain ◽

Methicillin Resistant ◽

Activity Evaluation

Monofluoro- (39), difluoro- (40) and trifluoro- (41) substituted analogues showed different biological activities, and 40 is a potent antibacterial agent in animal models.

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Bioactive Secondary Metabolites from the Mangrove Endophytic Fungi Nigrospora oryzae

Indonesian Journal of Chemistry ◽

10.22146/ijc.63129 ◽

2021 ◽

Vol 21 (4) ◽

pp. 1016

Author(s):

Antonius Rolling Basa Ola ◽

Titus Lapailaka ◽

Hermania Em Wogo ◽

Julinda Bendalina Dengga Henuk ◽

Agnes Simamora ◽

...

Keyword(s):

Secondary Metabolites ◽

Endophytic Fungi ◽

Antibacterial Agent ◽

Mangrove Forest ◽

Chemical Investigation ◽

Terrestrial Environment ◽

Agent Based ◽

Bioactive Secondary Metabolites ◽

Nigrospora Oryzae

Mangrove forest has a distinctive habitat adapting with marine and terrestrial environment. Chemical investigation of the extract from mangrove endophytic fungi Nigrospora oryzae had resulted in the isolation of sterigmatocystin (1) and pestalopyrone (2). The structure of sterigmatocystin (1) and pestalopyrone (2) were elucidated using mass, UV and NMR spectrometers together with the comparison with the literature data. The study also showed that sterigmatocystin displayed moderate cytotoxicity but it could be further developed as antiviral and antibacterial agent based on the SAR information reported from its analogue and derivatives.

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Carbonated Hydroxyapatite Containing Propolis as an Antibacterial Agent Candidate against Aggregatibacter actinomycetemcomitans

Majalah Obat Tradisional ◽

10.22146/mot.62712 ◽

2020 ◽

Vol 25 (3) ◽

Author(s):

Ayunda Nur Sukmawati ◽

Sri Pramestri ◽

Al. Sri Koes Soesilowati ◽

Suryono Suryono

Keyword(s):

Antibacterial Activity ◽

Bacterial Adhesion ◽

Antibacterial Agent ◽

Alveolar Bone ◽

Inhibition Zone ◽

Aggregatibacter Actinomycetemcomitans ◽

Test Method ◽

Graft Material ◽

Carbonated Hydroxyapatite ◽

Significant Difference

One of the periodontal pathogenic bacteria that can cause periodontitis and alveolar bone destruction is Aggregatibacter actinomycetemcomitans. An alveolar bone defect can be treated using a bone graft. Carbonated hydroxyapatite (CHA) is an alloplastic graft material. Alloplastic materials do not have vascularization, which will increase the risk of bacterial adhesion. Therefore, adding an antibacterial agent is needed to prevent bacterial adhesion, which will improve periodontal healing. Propolis is a natural ingredient that has broad-spectrum antibacterial activity and does not cause bacterial resistance. This study aimed to assess the antibacterial activity of carbonated hydroxyapatite after being incorporated with propolis against Aggregatibacter actinomycetemcomitans. Carbonated hydroxyapatite was embedded into four different concentrations of propolis solution (2.5%, 5%, 7.5%, and 10%). An antimicrobial assay against Aggregatibacter actinomycetemcomitans was done using the disc diffusion test method. The inhibition zone was measured to determine the antibacterial ability of the specimens. The inhibition zone was found on the carbonated hydroxyapatite incorporated with propolis at all concentrations. Carbonated hydroxyapatite incorporated with 10% propolis showed the largest inhibition zone. Data analysis using the Kruskal–Wallis test showed a significant difference between the groups tested (p <.05). In conclusion, carbonated hydroxyapatite incorporated with propolis has antibacterial activity against Aggregatibacter actinomycetemcomitans

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