ChemInform Abstract: Synthesis, Characterization and Antibacterial Activity of Benzimidazole Derivatives Carrying Quinoline Moiety.

ChemInform ◽  
2012 ◽  
Vol 43 (7) ◽  
pp. no-no
Author(s):  
Janardhana Gowda ◽  
A. M. A. Khader ◽  
Balakrishna Kalluraya ◽  
Syed Hidayathulla
Keyword(s):  
Antibacterial Activity ◽  
Benzimidazole Derivatives ◽  
Quinoline Moiety

scholarly journals Synthesis, in silico studies and antibacterial activity of some novel 2-substituted benzimidazole derivatives

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Ramakrishna Chintakunta ◽  
Geethavani Meka
Keyword(s):  
Antibacterial Activity ◽  
Melting Point ◽  
In Silico ◽  
Software Tool ◽  
Benzimidazole Derivatives ◽  
Recrystallization Process ◽  
Standard Drug ◽  
In Silico Studies ◽  
Drug Synthesis ◽  
Percentage Absorption

Abstract Background The o-phenylenediamine is a versatile starting material for several compounds. Synthesized o-phenylenediamine and amino acids (glycine, alanine, aspartic acid, and l-proline) undergo condensation via Phillips reaction. The synthesized compound showed the promising antibacterial activity of Bacillus subtilis and Pseudomonas aeruginosa at the concentration of 100, 50, 25, 12.5, 6.25, 3.12, 1.6, 0.8, 0.4, and 0.2 μg/ml. Ciprofloxacin was used as standard drug. Synthesis of benzimidazole derivatives was carried out and purified by recrystallization process using ethanol. Substituted derivatives were characterized by melting point, TLC and spectroscopic methods include FT-IR and 1H-NMR. Results In silico studies were adopted for synthetic derivatives by Molinspiration, ChemDraw, and online software tool. Minimum inhibitory concentration (MIC) values of B. subtilis and P. aeruginosa were reported, and benzimidazole ligands and Molinspiration scores were generated and listed. Conclusion The more negative values indicate a higher binding affinity. The generated ligand observations can be visualized. Physical constants of synthesized derivates such as solubility and melting point were determined. Bioactivity scores were noted for different derivatives and predicted percentage absorption in the gut. The antibacterial activity was performed using the MIC method (aerobic).

scholarly journals QSAR modeling of antibacterial activity of some benzimidazole derivatives

2011 ◽  
Vol 17 (1) ◽  
pp. 33-38 ◽  
Author(s):  
Sanja Podunavac-Kuzmanovic ◽  
Dragoljub Cvetkovic
Keyword(s):  
Antibacterial Activity ◽  
Qsar Model ◽  
Quantitative Structure Activity Relationship ◽  
Structural Features ◽  
Benzimidazole Derivatives ◽  
Qsar Modeling ◽  
Qsar Study ◽  
Validation Procedure ◽  
Leave One Out

A quantitative structure-activity relationship (QSAR) study has been carried out for training set of 12 benzimidazole derivatives to correlate and predict the antibacterial activity of studied compounds against Gram-negative bacteria Pseudomonas aeruginosa. Multiple linear regression was used to select the descriptors and to generate the best prediction model that relates the structural features to inhibitory activity. The predictivity of the model was estimated by cross-validation with the leave-one-out method. Our results suggest a QSAR model based on the following descriptors: parameter of lipophilicity (logP) and hydration energy (HE). Good agreement between experimental and predicted inhibitory values, obtained in the validation procedure, indicated the good quality of the generated QSAR model.

SYNTHESIS AND EVALUATION OF ANTIBACTERIAL, ANTHELMINTIC ACTIVITIES OF SUBSTITUTED BENZIMIDAZOLE DERIVATIVES

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (06) ◽  
pp. 69-76
Author(s):  
D Sharma ◽  
◽  
G. K Sharma ◽  
D. Pathak ◽  
M. C. Sharma
Keyword(s):  
Antibacterial Activity ◽  
Anthelmintic Activity ◽  
Benzimidazole Derivatives ◽  
The Novel ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Alkyl Aryl ◽  
Gram Negative ◽  
E Coli

The study was undertaken to synthesize and evaluate antibacterial, anthelmintic activities of N’ (substituted benzylidene)-2-(2-alkyl/aryl-1H-benzo[d] imidazole-1yl) acetohydrazide derivatives. All the novel benzimidazole derivatives were screened for anthelmintic activity against Pherituma posthuma species of earthworms and antibacterial activity against following bacterial strains: S. aureus, B.subtilis (Gram positive) and E. coli and P.aeruginosa (Gram negative). The antibacterial data suggest that compounds having nitro and hydroxyl substitution were more potent and the anthelmintic data suggest that compounds having chloro were most active.

scholarly journals Antibacterial activity of cobalt(II) complexes with some benzimidazole derivatives

2008 ◽  
Vol 73 (12) ◽  
pp. 1153-1160 ◽  
Author(s):  
S.O. Podunavac-Kuzmanovic ◽  
V.M. Leovac ◽  
D.D. Cvetkovic
Keyword(s):  
Antibacterial Activity ◽  
Chemical Structure ◽  
Antibacterial Activities ◽  
Benzimidazole Derivatives ◽  
Wall Structure ◽  
Gram Negative Bacteria ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative

The antibacterial activities of cobalt(II) complexes with two series of benzimidazoles were evaluated in vitro against three Gram-positive bacterial strains (Bacillus cereus, Staphylococcus aureus, and Sarcina lutea) and one Gram-negative isolate (Pseudomonas aeruginosa). The minimum inhibitory concentration was determined for all the complexes. The majority of the investtigated complexes displayed in vitro inhibitory activity against very persistent bacteria. They were found to be more active against Gram-positive than Gram-negative bacteria. It may be concluded that the antibacterial activity of the compounds is related to the cell wall structure of the tested bacteria. Comparing the inhibitory activities of the tested complexes, it was found that the 1-substituted- -2-aminobenzimidazole derivatives were more active than complexes of 1-substituted- 2-amino-5,6-dimethylbenzimidazoles. The effect of chemical structure on the antibacterial activity is discussed.

scholarly journals Synthesis, antiprotozoal and antibacterial activity of nitro- and halogeno-substituted benzimidazole derivatives.

2002 ◽  
Vol 49 (1) ◽  
pp. 185-195 ◽  
Author(s):  
Zygmunt Kazimierczuk ◽  
Jacqueline A Upcroft ◽  
Peter Upcroft ◽  
Agata Górska ◽  
Bohdan Starościak ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Benzimidazole Derivatives ◽  
Gram Negative Bacteria ◽  
Antiprotozoal Activity ◽  
Gram Positive ◽  
Gram Negative

Two series of benzimidazole derivatives were sythesised. The first one was based on 5,6-dinitrobenzimidazole, the second one comprises 2-thioalkyl- and thioaryl-substituted modified benzimidazoles. Antibacterial and antiprotozoal activity of the newly obtained compounds was studied. Some thioalkyl derivatives showed remarkable activity against nosocomial strains of Stenotrophomonas malthophilia, and an activity comparable to that of metronidazole against gram-positive and gram-negative bacteria. Of the tested compounds, 5,6-dichloro-2-(4-nitrobenzylthio)-benzimidazole showed the most distinct antiprotozoal activity.

scholarly journals Prediction of the inhibitory activity of benzimidazole derivatives against Bacillus spp.

2011 ◽  
pp. 251-261 ◽  
Author(s):  
Sanja Podunavac-Kuzmanovica ◽  
Dragoljub Cvetkovic ◽  
Slobodan Gadzuric
Keyword(s):  
Antibacterial Activity ◽  
Quantitative Structure Activity Relationship ◽  
Benzimidazole Derivatives ◽  
Calibration Model ◽  
Statistical Parameters ◽  
Gram Positive Bacteria ◽  
Bacillus Spp ◽  
In Vitro Antibacterial Activity ◽  
Leave One Out

In the present paper, the antibacterial activity of some 1-benzylbenzimidazole derivatives was evaluated against Gram-positive bacteria Bacillus spp. by using QSAR (quantitative structure-activity relationship). The tested compounds displayed in vitro antibacterial activity and minimum inhibitory concentration (MIC) was determined for all compounds. The lipophilicity descriptors of the studied compounds were measured by theoretical calculation (ClogP). The correlation between the MIC (log1/cMIC) and lipophilicity descriptors was investigated, and a mathematical model has been developed as a calibration model for predicting the antibacterial activity of this class of compounds. The quality of the model was validated by leave one out (LOO) technique as well as by the calculation of statistical parameters for the established model. The results of the present study may be useful for the designing of new benzimidazole derivatives that would be more potent against Bacillus spp.

scholarly journals Application of QSAR models in analysis of antibacterial activity of some benzimidazole derivatives against Sarcina lutea

2013 ◽  
Vol 67 (1) ◽  
pp. 27-33
Author(s):  
Sanja Podunavac-Kuzmanovic ◽  
Dragoljub Cvetkovic ◽  
Lidija Jevric ◽  
Natasa Uzelac
Keyword(s):  
Antibacterial Activity ◽  
Inhibitory Activity ◽  
Antibacterial Activities ◽  
Quantitative Structure Activity Relationship ◽  
Benzimidazole Derivatives ◽  
Log P ◽  
Statistical Parameters ◽  
Qsar Analysis ◽  
Qsar Models

In the present paper, a quantitative structure activity relationship (QSAR) has been carried out on a series of 2-methyl and 2-aminobenzimidazole derivatives to identify the lipophilicity requirements for their inhibitory activity against bacteria Sarcina lutea. The tested compounds displayed in vitro antibacterial activity and minimum inhibitory concentration (MIC) was determined for all compounds. The partition coefficients of the studied compounds were measured by the shake flask method (log P) and by theoretical calculation (Clog P). The relationships between lipophilicity descriptors and antibacterial activities were investigated and the mathematical models have been developed as a calibration models for predicting the inhibitory activity of this class of compounds. The models were validated by leave-one-out (LOO) technique as well as by the calculation of statistical parameters for the established models. Therefore, QSAR analysis reveals that lipophilicity descriptor govern the inhibitory activity of benzimidazoles studied against Sarcina lutea.

scholarly journals Quantitative structure-activity relationships to predict antibacterial effect of some benzimidazole derivatives

2008 ◽  
pp. 181-191 ◽  
Author(s):  
Sanja Podunavac-Kuzmanovic ◽  
Dijana Barna ◽  
Dragoljub Cvetkovic
Keyword(s):  
Antibacterial Activity ◽  
Qsar Model ◽  
Quantitative Structure Activity Relationship ◽  
Biologically Active ◽  
Benzimidazole Derivatives ◽  
Quantitative Structure ◽  
Structure Activity ◽  
Lipophilicity Parameter ◽  
Office Software

The antibacterial activity of some substituted benzimidazole derivatives against Gram negative bacteria Escherichia coli was investigated. The tested compounds displayed in vitro inhibitory activity and their minimum inhibitory concentrations were determined. Quantitative structure-activity relationship has been used to study the relationships between the antibacterial activity and lipophilicity parameter, logP. Lipophilicity parameters were calculated for each molecule by using CS Chem-Office Software version 7.0. Multiple linear regression was used to correlate the logP values and antibacterial activity of benzimidazole derivatives. The results are discussed on the basis of statistical data. The most acceptable QSAR model for prediction of antibacterial activity of the investigated series of benzimidazoles was developed. High agreement between experimental and predicted inhibitory values was obtained. The results of this study indicate that the lipophilicity parameter has a significant effect on antibacterial activity of this class of compounds, thus simplifying design of new biologically active molecules.

scholarly journals Design, Synthesis and <i>in Vitro</i> Antibacterial Activity of 2-thiomethyl-benzimidazole Derivatives

2021 ◽  
Vol 11 (04) ◽  
pp. 165-177
Author(s):  
Ablo Evrard ◽  
Coulibali Siomenan ◽  
Camara Tchambaga Etienne ◽  
Toure Daouda ◽  
Coulibaly Souleymane ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Benzimidazole Derivatives ◽  
Design Synthesis

scholarly journals The effect of lipophilicity on the antibacterial activity of some 1-benzylbenzimidazole derivatives

2008 ◽  
Vol 73 (10) ◽  
pp. 967-978 ◽  
Author(s):  
S.O. Podunavac-Kuzmanovic ◽  
D.D. Cvetkovic ◽  
D.J. Barna
Keyword(s):  
Antibacterial Activity ◽  
Quantitative Structure Activity Relationship ◽  
Biologically Active ◽  
Benzimidazole Derivatives ◽  
Log P ◽  
P Values ◽  
High Agreement ◽  
Software Products ◽  
Lipophilicity Parameter ◽  
Qsar Models

In the present paper, the antibacterial activity of some 1-benzylbenzimidazole derivatives were evaluated against the Gram-negative bacteria Escherichia coli. The minimum inhibitory concentration was determined for all the compounds. Quantitative structure-activity relationship (QSAR) was employed to study the effect of the lipophilicity parameters (log P) on the inhibitory activity. Log P values for the target compounds were experimentally determined by the "shake-flask" method and calculated by using eight different software products. Multiple linear regression was used to correlate the log P values and antibacterial activity of the studied benzimidazole derivatives. The results are discussed based on statistical data. The most acceptable QSAR models for the prediction of the antibacterial activity of the investigated series of benzimidazoles were developed. High agreement between the experimental and predicted inhibitory values was obtained. The results of this study indicate that the lipophilicity parameter has a significant effect on the antibacterial activity of this class of compounds, which simplifies the design of new biologically active molecules.

Sign in / Sign up

Export Citation Format

Share Document