scholarly journals Design, Synthesis and Antibacterial Activity of Coumarin-1,2,3-triazole Hybrids Obtained from Natural Furocoumarin Peucedanin

Molecules ◽  
2019 ◽  
Vol 24 (11) ◽  
pp. 2126 ◽  
Author(s):  
Alla V. Lipeeva ◽  
Danila O. Zakharov ◽  
Liubov G. Burova ◽  
Tatyana S. Frolova ◽  
Dmitry S. Baev ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Cycloaddition Reaction ◽  
Bacterial Strains ◽  
Design Synthesis ◽  
Docking Simulations ◽  
E Coli ◽  
Antibiotic Drugs ◽  
In Vitro Antibacterial Activity ◽  
Substituted Coumarins

Synthesis of 1,2,3-triazole-substituted coumarins and also 1,2,3-triazolyl or 1,2,3-triazolylalk-1-inyl-linked coumarin-2,3-furocoumarin hybrids was performed by employing the cross-coupling and copper catalyzed azide-alkyne cycloaddition reaction approaches. The synthesized compounds were evaluated for their in vitro antibacterial activity against Staphylococcus aureus, Bacillius subtilis, Actinomyces viscosus and Escherichia coli bacterial strains. Coumarin-benzoic acid hybrids 4с, 42с and 3-((4-acetylamino-3-(methoxycarbonyl)phenyl)ethynyl)coumarin (29) showed promising activity against S. aureus strains, and the 1,2,3-triazolyloct-1-inyl linked coumarin-2,3-furocoumarin hybrid 37c was endowed with high selectivity against B. subtilis and E. coli species. The in vitro antibacterial activity of 4с, 29, 37c and 42с can potentially be compared with that of a number of modern antibiotic drugs used in the clinic, suggesting promising prospects for further research. A detailed study of the molecular interactions with the targeted protein MurB was performed using docking simulations and the obtained results are quite promising.

scholarly journals Design, Synthesis and Antibacterial Evaluation of 3-Substituted Ocotillol-Type Derivatives

Molecules ◽  
2018 ◽  
Vol 23 (12) ◽  
pp. 3320 ◽  
Author(s):  
Kai-Yi Wang ◽  
Zhi-Wen Zhou ◽  
Heng-Yuan Zhang ◽  
Yu-Cheng Cao ◽  
Jin-Yi Xu ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Triterpenoid Saponin ◽  
Bacterial Strains ◽  
Design Synthesis ◽  
Design And Synthesis ◽  
Good Antibacterial Activity ◽  
Structure Activity ◽  
In Vitro Antibacterial Activity ◽  
Free Hydroxyl

Antibiotic resistance has become a serious global problem that threatens public health. In our previous work, we found that ocotillol-type triterpenoid saponin showed good antibacterial activity. Based on preliminary structure-activity relationship, novel serious C-3 substituted ocotillol-type derivatives 7–26 were designed and synthesized. The in vitro antibacterial activity was tested on five bacterial strains (B. subtilis 168, S. aureus RN4220, E. coli DH5α, A. baum ATCC19606 and MRSA USA300) and compared with the tests on contrast. Among these derivatives, C-3 position free hydroxyl substituted compounds 7–14, showed good antibacterial activity against Gram-positive bacteria. Furthermore, compound 22 exhibited excellent antibacterial activity with minimum inhibitory concentrations (MIC) values of 2 μg/mL against MRSA USA300 and 4 μg/mL against B. subtilis. The structure-activity relationships of all current ocotillol-type derivatives our team synthesised were summarized. In addition, the prediction of absorption, distribution, metabolism, and excretion (ADME) properties and the study of pharmacophores were also conducted. These results can provide a guide to further design and synthesis works.

scholarly journals In Vitro Antibacterial Activity of Black Soldier Fly (Hermetia Illucens) Larva Extracts Against Gram-Negative Bacteria

2019 ◽  
Vol 43 (2) ◽  
Author(s):  
Harlystiarini Harlystiarini ◽  
Rita Mutia ◽  
I Wayan Teguh Wibawan ◽  
Dewi Apri Astuti
Keyword(s):  
Antibacterial Activity ◽  
Inhibition Zone ◽  
Test Method ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Black Soldier Fly ◽  
E Coli ◽  
In Vitro Antibacterial Activity ◽  
Zone Growth

The aim of this study was to evaluate the in vitro antibacterial activity of Black soldier fly (BSF) larva extract. The BSF larva was extracted using methanol and then tested for antibacterial activity using agar diffusion method (zone growth inhibition). The antibacterial activity was conducted against Salmonella sp. and Escherichia coli, two important bacterial strains in poultry, using six dilution levels (10 mg/ml, 20 mg/ml, 40 mg/ml, 80 mg/ml, 160 mg/ml and 320 mg/ml). All the results were subjected analyze using t-test method. Based on the diameter of the inhibition zone, the BSF larva extract has a strong (P<0.05) antibacterial activity against Salmonella sp. and E. coli when the concentration used 320 mg/ml. In addition, BSF larva extract also contain high amount of lauric acid (49.18%), a saturated fatty acid that has been proven to proposes as antibacterial agent. Therefore, it could be concluded that the BSF larva extract could be used as a candidate for antibacterial substances. 

scholarly journals Phytochemical characterization and in vitro antibacterial activity of Xeroderris stuhlmannii (Taub.) Mendonca & E.P. Sousa bark extracts

2020 ◽  
Author(s):  
Major A. Selemani ◽  
Luckmore F. Kazingizi ◽  
Emily Manzombe ◽  
Lorraine Y. Bishi ◽  
Cleopas Mureya ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Rural Communities ◽  
Generic Drugs ◽  
Bark Extract ◽  
Herbal Supplement ◽  
Bacterial Strains ◽  
E Coli ◽  
In Vitro Antibacterial Activity ◽  
Phytochemical Compounds

ABSTRACTThe use of herbal medicine is common in many rural communities in Zimbabwe because generic drugs are expensive and not readily available. In this work, we documented the important phytochemicals from Xeroderris stuhlmannii (Taub.) Mendonca & E.P. Sousa (Murumanyama in Shona), bark extracts and tested their antibacterial activity in order to demonstrate its potential as an antimicrobial agent. Qualitative screening of secondary metabolites confirmed the presence of alkaloids, flavonoids, terpenoids, steroids and polyphenols in the crude bark extracts. The MICs values for the crude extracts on six bacterial strains ranged from 0.23–0.80 mg/mL. Antimicrobial tests showed higher potency for crude bark extracts on E. Coli (MIC, 0.232 mg/mL) and lower potency on coliform (MIC, 0.798 mg/mL). LC-MS/MS analysis of various fractions confirmed the presence of twenty-eight phytochemicals whereas, twelve phytochemicals were identified using GC-MS. Both techniques confirmed the presence of ursolic acid, roburic acid, reticuline, rotenone and p-coumaric acid glucoside in hexane and methanol extracts. In summary, our findings show that Xeroderris stuhlmannii (Taub.) Mendonca & E.P. Sousa contain many phytochemical compounds that have antimicrobial activity. Moreover, some of the compounds in the bark extract have been shown to possess antioxidant, antiviral, antitumor and anti-inflammatory properties. Thus, Xeroderris stuhlmannii (Taub.) Mendonca & E.P. Sousa barks can act as a useful herbal supplement for treatment of a number of diseases in rural communities where modern drugs are expensive and not readily available.

In Vitro Antibacterial activity of ethanolic extract of Myrsine africana against laboratory Strains of Pathogenic Organisms

2016 ◽  
Vol 5 (04) ◽  
pp. 4512
Author(s):  
Jackie K. Obey ◽  
Anthoney Swamy T* ◽  
Lasiti Timothy ◽  
Makani Rachel
Keyword(s):  
Antibacterial Activity ◽  
Minimum Inhibitory Concentration ◽  
Inhibitory Concentration ◽  
Ethanolic Extract ◽  
Ethanol Extract ◽  
E Coli ◽  
Zones Of Inhibition ◽  
In Vitro Antibacterial Activity ◽  
Myrsine Africana

The determination of the antibacterial activity (zone of inhibition) and minimum inhibitory concentration of medicinal plants a crucial step in drug development. In this study, the antibacterial activity and minimum inhibitory concentration of the ethanol extract of Myrsine africana were determined for Escherichia coli, Bacillus cereus, Staphylococcus epidermidis and Streptococcus pneumoniae. The zones of inhibition (mm±S.E) of 500mg/ml of M. africana ethanol extract were 22.00± 0.00 for E. coli,20.33 ±0.33 for B. cereus,25.00± 0.00 for S. epidermidis and 18. 17±0.17 for S. pneumoniae. The minimum inhibitory concentration(MIC) is the minimum dose required to inhibit growth a microorganism. Upon further double dilution of the 500mg/ml of M. africana extract, MIC was obtained for each organism. The MIC for E. coli, B. cereus, S. epidermidis and S. pneumoniae were 7.81mg/ml, 7.81mg/ml, 15.63mg/ml and 15.63mg/ml respectively. Crude extracts are considered active when they inhibit microorganisms with zones of inhibition of 8mm and above. Therefore, this study has shown that the ethanol extract of M. africana can control the growth of the four organisms tested.

scholarly journals Design, Synthesis and Biological Evaluation of Novel Benzothiazole Based [1,2,4]Triazolo[4,3-c]quinazoline Derivatives

2020 ◽  
Vol 32 (3) ◽  
pp. 580-586
Author(s):  
Ranjit V. Gadhave ◽  
Bhanudas S. Kuchekar
Keyword(s):  
Biological Evaluation ◽  
Bacterial Strains ◽  
Active Compounds ◽  
Design Synthesis ◽  
Structural Modifications ◽  
E Coli ◽  
Chemical Structures ◽  
Ft Ir ◽  
Antioxidant Agent

A new series of N-(benzo[d]thiazol-2-yl)-[1,2,4]triazolo[4,3-c]quinazoline-5-carboxamide derivatives were synthesized by condensation of [1,2,4]triazolo[4,3-c]quinazoline-5-carboxylate derivatives with substituted benzothiazoles. The chemical structures of the synthesized compounds were confirmed by FT-IR, MS and 1H NMR spectra. Designed triazoloquinazoline derivatives were docked with oxido-reductase enzyme (PDB Code 4h1j) and DNA gyrase enzyme (PDB Code 3g75). Based on high binding affinity score, the best compound were selected for synthesis and subjected to in vitro antioxidant and antibacterial activity. Compounds 7a and 7d were found to be most active compounds as antioxidant agent among this series when compared with ascorbic acid. Compounds 7a, 7d and 7f were found to be most active compounds as an antibacterial agents among this series when compared with ciprofloxacin against bacterial strains such as S. aureus (ATCC 25923), E. coli (ATCC 25922) and P. aeruginosa (ATCC 27853). Study revealed that the most active compounds after structural modifications can be exploited as lead molecules for other pharmacological activities such as anti-inflammatory, anticancer and antidepressant activities.

Design, synthesis and antibacterial evaluation of ocotillol derivatives with polycyclic nitrogen-containing groups

2021 ◽  
Author(s):  
Yucheng Cao ◽  
Kaiyi Wang ◽  
Jiali Wang ◽  
Haoran Cheng ◽  
Mengxin Ma ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Multidrug Resistant ◽  
Inhibitory Effect ◽  
Resistant Bacteria ◽  
Design Synthesis ◽  
In Vitro Antibacterial Activity ◽  
Strong Inhibitory Effect ◽  
Hospital Acquired ◽  
Derivatives Of

Aim: With the increasing abuse of antibacterial drugs, multidrug-resistant bacteria have become a burden on human health and the healthcare system. To find alternative compounds effective against hospital-acquired methicillin-resistant Staphylococcus aureus (HA-MRSA), novel derivatives of ocotillol were synthesized. Methods & Results: Ocotillol derivatives with polycyclic nitrogen-containing groups were synthesized and evaluated for in vitro antibacterial activity. Compounds 36–39 exhibited potent antibacterial activity against hospital-acquired MRSA, with MIC = 8–64 μg/ml. Additionally, a combination of compound 37 and the commercially available antibiotic kanamycin showed synergistic inhibitory effects, with a fractional inhibitory concentration index of ≤0.375. Conclusion: Compound 37 has a strong inhibitory effect, and this derivative has potential for use as a pharmacological tool to explore antibacterial mechanisms.

scholarly journals In Vitro Antibacterial Activity of an Aqueous Extracts of the Tephrosia Vogelii Hook.f Combined To Imipenem on E. coli Strains

2020 ◽  
Vol 09 (01) ◽  
pp. 36-45
Author(s):  
 Jean Fabrice Yala ◽  
Rolande Mabika Mabika ◽  
Franck Mounioko ◽  
Ornella Zong Minko ◽  
Alexis Nicaise Lepengue ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Aqueous Extracts ◽  
E Coli ◽  
Tephrosia Vogelii ◽  
In Vitro Antibacterial Activity

scholarly journals In vitro Evaluationof the Antimi- crobial Activity of a Topical Skin Preparation Containing 0.1% Polyhexanide vs a Topical Skin Prepa-ration Containing 1% Silver Sulfadiazine

2021 ◽  
Vol 6 (2) ◽  
pp. 1-7
Author(s):  
Barbara Maglione ◽  
Keyword(s):  
Antibacterial Activity ◽  
Positive Control ◽  
Negative Control ◽  
Silver Sulfadiazine ◽  
Bacterial Strains ◽  
Skin Preparation ◽  
E Coli ◽  
Topical Cream ◽  
Significant Difference

Aim: The effective in vitro antibacterial activity on Staphylococcus aureus (S.aureus), Pseudomonas aeruginosa (P.aeruginosa), Klebsiella pneumoniae (K.pneumoniae),Escherichia coli (E.Coli) and the combination of S.aureus and K. pneumonia of a topical cream based on 0.1% polyhexanidewas compared to a topical cream based on 1% silver sulfadiazine.A topical cream containing 0,1% gentamicin was used as a positive control and a white blank topical cream was used as negative control. Materials and Methods: The in vitro antibacterial activities were determined by agar well-diffusion assay. Two-way Analysis of Variance (ANOVA) was used to test, by calculation of P-values, for significant antiseptic activity in bacteria treated with 0.1% polyhexanide topical cream compared to 1% silver sulfadiazine and to the negative and positive controls. Results: Among the derivatives tested, all the active topical creams analyzed were able to reduce microbial strains. The topical cream based on 0.1% polyhexanide showed a significantly higher antibacterial efficacy in comparison to the topical cream based on 1% silver sulfadiazine on S. aureus and K. pneumonia and on the combination of S. aureus and K. pneumoniae,while no significant difference was detected between the antibacterial activity of the two topical creams against P. aeruginosa and E. coli. Conclusion: These results provide a further insight into the antibacterial activity of polyhexanide and its non-inferiority compared to silver sulfadiazine towards certain bacterial strains (P. aeruginosa and E. coli) and superiority towards other (S. aureus and K. pneumoniae)and support the use of 0.1% Polyhexanide topical preparation for the treatment of wounds that are infected or at risk of infection.

scholarly journals β-Lactamase inhibition profile of new amidine-substituted diazabicyclooctanes

2021 ◽  
Vol 17 ◽  
pp. 711-718
Author(s):  
Zafar Iqbal ◽  
Lijuan Zhai ◽  
Yuanyu Gao ◽  
Dong Tang ◽  
Xueqin Ma ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Second Generation ◽  
Bacterial Species ◽  
The Other ◽  
Inhibition Activity ◽  
Bacterial Strains ◽  
E Coli ◽  
Mic Value

The diazabicyclooctane (DBO) scaffold is the backbone of non-β-lactam-based second generation β-lactamase inhibitors. As part of our efforts, we have synthesized a series of DBO derivatives A1–23 containing amidine substituents at the C2 position of the bicyclic ring. These compounds, alone and in combination with meropenem, were tested against ten bacterial strains for their antibacterial activity in vitro. All compounds did not show antibacterial activity when tested alone (MIC >64 mg/L), however, they exhibited a moderate inhibition activity in the presence of meropenem by lowering its MIC values. The compound A12 proved most potent among the other counterparts against all bacterial species with MIC from <0.125 mg/L to 2 mg/L, and is comparable to avibactam against both E. coli strains with a MIC value of <0.125 mg/L.

Sign in / Sign up

Export Citation Format

Share Document