scholarly journals Synthesis of new Imidazole Derivatives as effective Antimicrobial Agents

2017 ◽  
Vol 5 (01) ◽  
pp. 01-09
Author(s):  
Bipin Kumar Verma ◽  
Sunil Kapoor ◽  
Umesh Kumar ◽  
Savita Pandey ◽  
Priti Arya
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Micrococcus Luteus ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Mass Spectral ◽  
Analytical Technique ◽  
Imidazole Derivatives ◽  
Modern Analytical Technique ◽  
Anti Fungal

In the present work, some new imidazole derivatives (3i-xii) were synthesized as per design synthetic protocol scheme. The structures of newly prepared compounds were confirmed by modern analytical technique (IR, 1H-NMR, Mass spectral data) and elemental analysis, results found in full agreement with their assigned structures. All the synthetic compounds were screened for their antimicrobial activity against bacterial strains viz. Escherichia coli (E. coli, MTCC 2961), Staphylococcus aureus (S. aureus, MTCC 3160), Bacillus subtilis (B. subtilis, MTCC 121), Klebsiella pneumoniae (K. pneumoniae, MTCC 3040) and Micrococcus luteus (M. luteus, MTCC 7527)) and fungal strains viz. Candida albicans (C. albicans, MTCC 227), Aspergillus niger (A. niger, MTCC 277) and Aspergillus flavus (A. flavus, MTCC 418) ; results showed good to remarkable activity. The MIC (minimum inhibitory concentration) values were determined by comparison to ciprofloxacin (anti-bacterial) and fluconazole (anti-fungal) as standard drug. Among them, compound 3iv and 3x exhibited notable antimicrobial activity. These compounds may be used as new template for the searching of potential antimicrobial agents.

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF 3-FORMYL INDOLE BASED SCHIFF BASES

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Singh Gurvinder ◽  
Singh Prabhsimran ◽  
Dhawan R. K.
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Analysis ◽  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Fungal Strain ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Gram Negative ◽  
E Coli

In order to develop new antimicrobial agents, a series of 3-formyl indole based Schiff bases were synthesized by reacting 3-formyl indole(indole-3-carboxaldehyde) with substituted aniline taking ethanol as solvent. The reaction was carried in the presence of small amount of p-toluene sulphonic acid as catalyst.All the synthesized compounds were characterized by IR, 1H-NMR spectral analysis. All the synthesized compounds were evaluated for antimicrobial activity against two gram positive bacterial strains (B. subtilisand S. aureus) and two gram negative bacterial strains (P. aeruginosaand E. coli) and one fungal strain (C. albicans). All the synthesized compounds were found to have moderate to good antimicrobial activity. The  standard drug amoxicillin, fluconazole were used for antimicrobial activity. Among the synthesized compounds, the maximum antimicrobial activity was shown by compounds GS04, GS07, GS08 and GS10.

Highly Regioselective Ring-Opening of Epoxides: Synthesis and Biological Evaluation as Potent Antimicrobial Agents

2021 ◽  
Vol 6 (3) ◽  
pp. 228-234
Author(s):  
Nilam H. Lalavani ◽  
Krishna A. Bhensdadia ◽  
Shipra H. Baluja
Keyword(s):  
Ring Opening ◽  
Antimicrobial Agents ◽  
Catalytic Amount ◽  
Biological Evaluation ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Mass Spectral ◽  
Fungal Strains ◽  
Ring Opening Of Epoxides

In present work, a convenient method for the nucleophilic ring-opening of epoxides with secondary amine in presence of ethyl acetate as a polar aprotic solvent using catalytic amount of base is described. Present method is highly regioselective and furnishes the products in short time of period with excellent yield. The regioselectivity of this ring opening was confirmed using FT-IR, 1H NMR, 13C NMR, elemental analysis and mass spectral data. The antimicrobial screening of all these synthesized compounds was done against some bacterial and fungal strains in two polar solvents, DMSO and DMF using agar well diffusion method. These compounds showed good inhibition of bacterial strains and potent against fungal strains than standard drug.

scholarly journals Synthesis and Evaluation of Some Novel Chromone Based Dithiazoles as Antimicrobial Agents

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Naureen Aggarwal ◽  
Vishal Sharma ◽  
Harpreet Kaur ◽  
Mohan Paul Singh Ishar
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
Antimicrobial Agents ◽  
Fungal Strain ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Fungal Strains ◽  
Inhibitory Potential ◽  
C Nmr

Novel substituted 1,2,4-dithiazolylchromones 3a–j were synthesized by the reaction of 3-formylchromones (1a–j) with two equivalents of p-chlorothiobenzamide (2) in dry xylene and characterized spectroscopically (IR, 1H and 13C NMR, mass) and elemental analysis. All synthesized compounds were screened for in vitro antimicrobial activity against various pathogenic bacterial and fungal strains and were found to possess good to moderate inhibitory potential against all tested strains. Antimicrobial results reveal that compounds bearing lipophilic electron withdrawing groups such as chloro and bromo displayed significant inhibitory potential against both bacterial and fungal strains. Particularly, compound 3c displayed significant inhibitory against bacterial strains and compound 3h exhibits significant inhibitory potential in comparison to standard drug fluconazole against fungal strain S. cerevisiae.

scholarly journals Synthesis, Identification, Computer-Aided Docking Studies, and ADMET Prediction of Novel Benzimidazo-1,2,3-triazole Based Molecules as Potential Antimicrobial Agents

Molecules ◽  
2021 ◽  
Vol 26 (23) ◽  
pp. 7119
Author(s):  
Huda R. M. Rashdan ◽  
Aboubakr H. Abdelmonsef ◽  
Mortaga M. Abou-Krisha ◽  
Tarek A. Yousef
Keyword(s):  
Antimicrobial Activity ◽  
Binding Energy ◽  
Antimicrobial Agents ◽  
Sodium Ethoxide ◽  
Dna Gyrase ◽  
Docking Studies ◽  
Bacterial Strains ◽  
Standard Drug ◽  
E Coli

2-azido-1H-benzo[d]imidazole derivatives 1a,b were reacted with a β-ketoester such as acetylacetone in the presence of sodium ethoxide to obtain the desired molecules 2a,b. The latter acted as a key molecule for the synthesis of new carbazone derivatives 4a,b that were submitted to react with 2-oxo-N-phenyl-2-(phenylamino)acetohydrazonoyl chloride to obtain the target thiadiazole derivatives 6a,b. The structures of the newly synthesized compounds were inferred from correct spectral and microanalytical data. Moreover, the newly prepared compounds were subjected to molecular docking studies with DNA gyrase B and exhibited binding energy that extended from −9.8 to −6.4 kcal/mol, which confirmed their excellent potency. The compounds 6a,b were found to be with the minimum binding energy (−9.7 and −9.8 kcal/mol) as compared to the standard drug ciprofloxacin (−7.4 kcal/mol) against the target enzyme DNA gyrase B. In addition, the newly synthesized compounds were also examined and screened for their in vitro antimicrobial activity against pathogenic microorganisms Staphylococcus aureus, E. coli, Pseudomonas aeruginosa, Aspergillus niger, and Candida albicans. Among the newly synthesized molecules, significant antimicrobial activity against all the tested microorganisms was obtained for the compounds 6a,b. The in silico and in vitro findings showed that compounds 6a,b were the most active against bacterial strains, and could serve as potential antimicrobial agents.

scholarly journals Microwave Assisted Synthesis and Antimicrobial Evaluation of Schiff Bases of Indole-3-aldehyde

2011 ◽  
Vol 8 (1) ◽  
pp. 305-311 ◽  
Author(s):  
Priyanka Kamaria ◽  
N. Kawathekar ◽  
Prerna Chaturvedi
Keyword(s):  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Microwave Assisted Synthesis ◽  
Bacterial Strains ◽  
Mass Spectral Analysis ◽  
Gram Positive ◽  
Gram Negative ◽  
Mass Spectral ◽  
Microwave Assisted ◽  
Antimicrobial Evaluation

In order to develop new antimicrobial agents, a series of Schiff bases of indole-3-aldehyde were synthesized by microwave assisted synthesis by takingDMFas solvent and evaluated for their antimicrobial activity. All the synthesized compounds were characterized byIR,1HNMRand mass spectral analysis. All compounds were tested against five gram positive and five gram negative bacterial strains and one fungal strain. All compounds exhibited better activity against gram positive strains than against gram negative strains and the compounds were found more active againstS.aureusandB.subtilis.

scholarly journals Thymol and its Derivatives as Antimicrobial Agents

2008 ◽  
Vol 3 (5) ◽  
pp. 1934578X0800300 ◽  
Author(s):  
Ajai Kumar ◽  
Suriya P. Singh ◽  
Sudarshan S. Chhokar
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Single Step ◽  
Acid Chlorides ◽  
Disc Diffusion ◽  
Bacterial Strains ◽  
Fungal Strains ◽  
Broth Dilution

From the seeds of C arum copticum thymol (1) was isolated as the major component and ten derivatives (2–11) were prepared by reacting it with different acid chlorides in a single step. They were evaluated for antimicrobial activity against twelve bacterial strains and nine fungal strains using disc diffusion and broth dilution assays. Derivative 9 was found to be most active against both bacterial and fungal strains.

scholarly journals Chemical Composition and Antimicrobial Activity of the Essential Oil from Chaerophyllum Aureum L. (Apiaceae)

2009 ◽  
Vol 4 (1) ◽  
pp. 1934578X0900400 ◽  
Author(s):  
Branislava Lakušić ◽  
Violeta Slavkovska ◽  
Milica Pavlović ◽  
Marina Milenković ◽  
Jelena Antić Stanković ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Candida Albicans ◽  
Chemical Composition ◽  
Micrococcus Luteus ◽  
Bacterial Strains ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Aerial Parts

The essential oils of the aerial parts and fruits of Chaerophyllum aureum L., collected from two mountains in Serbia, were analyzed by GC and GC/MS. Sabinene (18.5-31.6%), p-cymene (7.9-25.4%) and limonene (1.9-10.9%) were characterized as the main constituents. The oils were tested against six bacterial strains and one strain of yeast, Candida albicans. The highest antimicrobial activity was observed against the Gram-positive bacteria Staphylococcus aureus, S. epidermidis and Micrococcus luteus, while of the Gram-negative strains, Escherichia coli was the most sensitive.

scholarly journals A Novel Hybrid Peptide Composed of LfcinB6 and KR-12-a4 With Enhanced Antimicrobial, Anti-Inflammatory and Anti-Biofilm Activities

2021 ◽  
Author(s):  
Chelladurai Ajish ◽  
Sungtae Yang ◽  
S. Dinesh Kumar ◽  
Eun Young Kim ◽  
Hye Jung Min ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Laser Scanning ◽  
Antimicrobial Agents ◽  
Laser Scanning Microscopy ◽  
Confocal Laser ◽  
Bacterial Cells ◽  
Bacterial Strains ◽  
Hybrid Peptide ◽  
Cell Selectivity ◽  
Anti Inflammatory

Abstract Hybridizing two known antimicrobial peptides (AMPs) is a simple and effective strategy for designing antimicrobial agents with enhanced cell selectivity against bacterial cells. Here, we generated a hybrid peptide Lf-KR in which LfcinB6 and KR-12-a4 were linked with a Pro hinge to obtain a novel AMP with potent antimicrobial, anti-inflammatory, and anti-biofilm activities. Lf-KR exerted superior cell selectivity for bacterial cells over sheep red blood cells. Lf-KR showed broad-spectrum antimicrobial activities (MIC: 4–8 mM) against tested 12 bacterial strains and retained its antimicrobial activity in the presence of salts at physiological concentrations. Membrane depolarization and dye leakage assays showed that the enhanced antimicrobial activity of Lf-KR was due to increased permeabilization and depolarization of microbial membranes. Lf-KR significantly inhibited the expression and production of pro-inflammatory cytokines (NO and TNF-a) in LPS-stimulated mouse macrophage RAW264.7 cells. In addition, Lf-KR showed a powerful eradication effect on preformed multidrug-resistant Pseudomonas aeruginosa (MDRPA) biofilms. We confirmed using confocal laser scanning microscopy that a large portion of the preformed MDRPA biofilm structure was perturbed by the addition of Lf-KR. Collectively, our results suggest that Lf-KR can be an antimicrobial, anti-inflammatory, and anti-biofilm candidate as a pharmaceutical agent.

scholarly journals A CLINICAL EVALUATION OF ANTIMICROBIAL ACTIVITY OF GOMUTRA ARKA IN DUSTA VRANA

2020 ◽  
pp. 27-35
Author(s):  
Manish Kumar Singh ◽  
P. Ramesh Bhat ◽  
Sweta Tyagi
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Povidone Iodine ◽  
Low Cost ◽  
P Value ◽  
Standard Drug ◽  
Classical Formulation ◽  
Group A ◽  
Group B ◽  
Trial Drug

Vrana chikitsha is very significant in field of Shalya tantra. Healing of Vrana is depends on many factors. Among them growth of microorganism play essential role to slow the process of healing. In Dusta Vrana to improve the healthy granulation and to reduce the colony count of microorganism specific Krimghna dravya is required for that in Shasthi upkrama under Krimighna karma Gomutra Arka is advised. Which has additional property of Lekhana and Ropana. Gomutra Arka is given importance in many oral classical formulation of Ayurveda to treat the Krimi, which is not evaluated for local application on Dusta Vrana yet. Materials and Methods: A simple randomized controlled clinical study where 50 patients were equally divided as group A: Gomutra Arka (trial drug) and Group B: Povidone-iodine (standard drug) for 14 days. Observations and results: The study result revealed that Gomutra Arka proved to be better Antimicrobial agents than povidone-iodine with a highly significant p-value of 0.04 in comparison to 0.68. It was also established in the study that 10mlGomutra Arka proved to be more effective on different microorganisms that are Staphylococcus Aureus, Pseudomonas Aeruginosa, Shigella, Salmonella, E. Coli, and Candida Albicans. Conclusion: The Gomutra Arka acts as an antimicrobial agent due to its property like Katu tikta kashya rasa which are Krimighna in nature by this inhibition of microorganism could happen also due to the Ushna tikshna and Kshara guna gives unfavorable environment for bacterial growth. The presence of constituents like copper, aurum, urea, ammonia further helps in antimicrobial activity. Therefore, Gomutra Arka can be used in regular practice as its available at a low cost, affordable and the study proves its efficiency over the Povidone-iodine controlled group.

scholarly journals Synthesis, antimicrobial and antimalarial activityof1, 4-benzothiazepine and pyrazolinederivatives incorporating carbazolemoiety

2019 ◽  
Vol 51 (2) ◽  
pp. 234-241
Author(s):  
V. A. Kadnor ◽  
S. N. Shelke
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
13C Nmr ◽  
Antimalarial Activity ◽  
Positive Control ◽  
Spectral Studies ◽  
Standard Drug ◽  
Mass Spectral ◽  
Ft Ir

A series of carbazole-based 1,4-benzothiazepine and pyrazoline derivatives were synthesized and the structures of the newly synthesized compounds were confirmed by FT-IR, 1H NMR, 13C NMR and mass spectral studies. All new derivatives 4(a-f) and 5(a-e) were screened for their in vitro antimicrobial activity, and also for their antimalarial activity. Compounds 4a, 4b, 4d, 5a, 5b and 5c exhibited promising antimicrobial and antimalarial activities as compared to positive control. Notably, compounds 4a, 4b and 4d showed excellent antifungal activity against Penicillium sp. comparable to that of a standard drug.

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