Synthesis and In Vitro Antimicrobial Evaluation of Hydrazones of 1-Phenyl-, 1-Benzyl-, and 1-Benzhydryl-4-aminopiperazines

1971 ◽  
Vol 60 (3) ◽  
pp. 386-389 ◽  
Author(s):  
D.K. Yung ◽  
D.E. Mahony ◽  
L.W. Whitehouse
Keyword(s):  
Antimicrobial Evaluation

scholarly journals Synthesis and In Vitro Antimicrobial Evaluation of Photoactive Multi—Block Chalcone Conjugate Phthalimide and 1,8-Naphthalimide Novolacs

Polymers ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1859
Author(s):  
Periyan Durairaju ◽  
Chinnasamy Umarani ◽  
Govindasami Periyasami ◽  
Perumberkandigai Adikesavan Vivekanand ◽  
Mostafizur Rahaman
Keyword(s):  
Spectroscopic Analysis ◽  
Photophysical Properties ◽  
Gel Permeation Chromatography ◽  
13C Nmr Spectroscopy ◽  
Antimicrobial Activities ◽  
Microbial Activities ◽  
E Coli ◽  
Molecular Weights ◽  
Antimicrobial Evaluation

Herein we report new multiblock chalcone conjugate phthalimide and naphthalimide functionalized copolymers with a topologically novel architecture synthesis using nucleophilic substitution and polycondensation methodology. The structures of the synthesized novolacs were elucidated on the basis of their spectroscopic analysis including FTIR, 1H NMR, and 13C NMR spectroscopy. Further, the number-average and weight-average molecular weights of the novolac polymers were determined by gel permeation chromatography (GPC). We examined the solubility of the synthesized polymers in various organic solvents including CHCl3, CH3CN, THF, H2O, CH3OH, DMSO, and DMF and found they are insoluble in both methanol and water. The novolac polymers were evaluated for their photophysical properties and microbial activities. The investigation of the antimicrobial activities of these polymers reveals significant antimicrobial activity against the pathogens E. coli, S. aureus, C. albicans, and A. niger.

scholarly journals Synthesis, Characterization and in vitro Antimicrobial Evaluation of Chalconeimine Derivatives as Potential Inhibitors against Enzymes Produced from S. aureus: A Computational Approach

2019 ◽  
Vol 31 (10) ◽  
pp. 2157-2164
Author(s):  
B. Prithivirajan ◽  
M. Jebastin Sonia Jas ◽  
G. Marimuthu
Keyword(s):  
Antibacterial Agents ◽  
Dna Gyrase ◽  
Bacterial Strains ◽  
Bacterial Proteins ◽  
Antibiotic Drug ◽  
In Vitro Antibacterial Activity ◽  
Antimicrobial Evaluation ◽  
Potential Inhibitors ◽  
Gyrase Inhibitors

(Z)-1-(Benzo[d][1,3]dioxol-5-yl)-3-(4-(difluoromethoxy)-3-hydroxyphenyl)prop-2-en-1-one hydrazone derivatives pronounced in this manuscript represents a new collection of antibacterial agents in addition to the DNA gyrase inhibitors. Efforts had been made to synthesize those chalcone-hydrazone derivatives (4a-e) in good yields. The literature survey confirms that nano-ZnO as heterogeneous catalyst has obtained big interest because of its ecofriendly nature and has been explored as a effective catalyst for several organic ameliorations. Subsequently, induced by way of these observations and in continuation to our interest in organic synthesis with using nanocatalyst. in vitro Antibacterial activity has been evaluated towards Gram-positive and Gram-negative bacterial strains for all compounds. So one can discover the affinity to bacterial proteins docking have a look at have been carried out for 5 synthesized derivatives, antibiotic drug and co-crystallized ligands with special mechanism of action DNA gyrase B and methylthioadenosine/S-adenosylhomocysteine nucleosidase (MTAN) the usage of AutoDock 4.

Potential bioactive mononuclear diorganotin(IV) phenoxyacetohydroxamate complexes: synthesis, characterization and antimicrobial evaluation

2018 ◽  
Vol 0 (0) ◽  
Author(s):  
Vineet Kumar Choudhary ◽  
Abhishek Kumar ◽  
Neeraj Sharma
Keyword(s):  
Antimicrobial Agents ◽  
Salmonella Typhi ◽  
Molar Ratio ◽  
Distorted Octahedral Geometry ◽  
Spectroscopic Techniques ◽  
Concentration Method ◽  
Distorted Octahedral ◽  
Elemental Analyses ◽  
Antimicrobial Evaluation

AbstractThe new diorganotin(IV) complexes of composition [Me2Sn(C6H5OCH2CONHO)2](I) and [n-Bu2Sn(C6H5OCH2CONHO)2](II) have been synthesized by the reactions of Me2SnCl2andn-Bu2SnCl2with potassium phenoxyacetohydroxamate (PhOAHK=C6H5OCH2CONHOK) in 1:2 molar ratio in methanol and benzene solvent medium and characterized by elemental analyses and spectroscopic techniques (infrared,1H nuclear magnetic resonance and mass spectrometry). The [O,O coordination] through carbonyl and hydroxamic oxygen atoms and distorted octahedral geometry around the mononuclear tin has been inferred. The electrochemical behavior of complexes studied by the cyclic voltammetric technique has shown quasi-irreversible two-step reduction from tin (IV) to tin (II). Thermal behavior of complexes studied by the thermogravimetric technique in N2atmosphere has yielded SnO as the decomposition product. Thein vitroantimicrobial activity assays against various pathogenic Gram-negative bacteria, namely,Salmonella typhi,Escherichia coli; Gram-positiveBacillus cereusandStaphylococcus aureusand fungiAspergillus nigerandAlternaria alternataby the minimum inhibitory concentration method have shown their potential as promising antimicrobial agents compared to the respective standard chloramphenicol and nystatin drugs.

Synthesis and antimicrobial activity of aryldiazenyl/arylhydrazono pyrazoles

2021 ◽  
Vol 45 (11-12) ◽  
pp. 1093-1099
Author(s):  
Abdulrhman Alsayari ◽  
Yahya I Asiri ◽  
Abdullatif Bin Muhsinah ◽  
Mohd. Zaheen Hassan
Keyword(s):  
Active Site ◽  
Phenyl Ring ◽  
Antimicrobial Agents ◽  
Inhibitory Concentration ◽  
Docking Studies ◽  
Considerable Effect ◽  
Design Synthesis ◽  
Structure Activity ◽  
Antimicrobial Evaluation

We report the design, synthesis, and in vitro antimicrobial evaluation of functionalized pyrazoles containing a hydrazono/diazenyl moiety. Among these newly synthesized derivatives, 4-[2-(4-chlorophenyl)hydrazono]-5-methyl-2-[2-(naphthalen-2-yloxy)acetyl]-2,4-dihydro-3 H-pyrazol-3-one is a promising antimicrobial agent against Staphylococcus aureus (minimum inhibitory concentration 0.19 μg mL−1). Structure–activity relationship studies reveal that the electronic environment on the distal phenyl ring has a considerable effect on the antimicrobial potential of the hybrid analogues. Molecular docking studies into the active site of S. aureus dihydrofolate reductase also prove the usefulness of hybridizing a pyrazole moiety with azo and hydrazo groups in the design of new antimicrobial agents.

scholarly journals Antimicrobial evaluation of methyl 4-O-Acetyl-α-L-Rhamnopyranoside derivatives

2013 ◽  
pp. 33-43
Author(s):  
Mohammed M Matin ◽  
Mohammad Ibrahim ◽  
Md Shafiqur Rahman
Keyword(s):  
Pathogenic Bacteria ◽  
Pathogenic Fungi ◽  
Macrophomina Phaseolina ◽  
Antibacterial Activities ◽  
Salmonella Typhi ◽  
Shigella Dysenteriae ◽  
Curvularia Lunata ◽  
In Vitro Antibacterial Activity ◽  
Antimicrobial Evaluation

A number of 2,3-di-O-acyl derivatives (6-11) of methyl 4-O-acetyl-a-Lrhamnopyranoside (5) obtained by using various acylating agents were screened for in vitro antifungal activity against four plant pathogenic fungi, viz., Alternaria alternata, Curvularia lunata. Fusarium equiseti and Macrophomina phaseolina. These compounds were also screened for in vitro antibacterial activity against ten human pathogenic bacteria, viz., Bacillus subtilis, Bacillus cereus, Bacillus megaterium, Staphylococcus aureus, Escherichia coli, INABA ET (Vibrio), Pseudomonas species, Salmonella paratyphi, Shigella dysenteriae and Salmonella typhi. The study reveal that these 4-O-acetyl-?-L-rhamnopyranoside derivatives are more prone towards antifungal activities than that of antibacterial activities. DOI: http://dx.doi.org/10.3329/cujbs.v3i1.13404 The Chittagong Univ. J. B. Sci.,Vol. 3(1&2):33-43, 2008

Design and Synthesis of Novel Sulfonamide-Derived Triazoles and Bioactivity Exploration

2020 ◽  
Vol 16 (1) ◽  
pp. 104-118 ◽  
Author(s):  
Shi-Chao He ◽  
Hui-Zhen Zhang ◽  
Hai-Juan Zhang ◽  
Qing Sun ◽  
Cheng-He Zhou
Keyword(s):  
Chlorosulfonic Acid ◽  
Antibacterial Activities ◽  
Structural Features ◽  
The Novel ◽  
E Coli ◽  
Design And Synthesis ◽  
Chemical Studies ◽  
Antimicrobial Evaluation ◽  
Better Than

Objective: Due to the incidence of resistance, a series of sulfonamide-derived 1,2,4- triazoles were synthesized and evaluated. Method: The novel sulfonamide-derived 1,2,4-triazoles were prepared starting from commercial acetaniline and chlorosulfonic acid by sulfonylation, aminolysis, N-alkylation and so on. The antimicrobial activity of the synthesized compounds were evaluated in vitro by two-fold serial dilution technique. Results: In vitro antimicrobial evaluation found that 2-chlorobenzyl sulfonamide 1,2,4-triazole 7c exhibited excellent antibacterial activities against MRSA, B. subtilis, B. typhi and E. coli with MIC values of 0.02−0.16 μmol/mL, which were comparable or even better than Chloromycin. The preliminary mechanism suggested that compound 7c could effectively bind with DNA, and also it could bind with human microsomal heme through hydrogen bonds in molecular docking. Computational chemical studies were performed on compound 7c to understand the structural features that are essential for activity. Additionally, compound 7c could generate a small amount of reactive oxygen species (ROS). Conclusion: Compound 7c could serve as a potential clinical antimicrobial candidate.

scholarly journals Design, Synthesis, and Antimicrobial Evaluation of New Annelated Pyrimido[2,1-c][1,2,4]triazolo[3,4-f][1,2,4]triazines

Molecules ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 1339 ◽  
Author(s):  
Islam H. El Azab ◽  
Nadia A.A. Elkanzi
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Positive Control ◽  
Design Synthesis ◽  
Aspergillus Brasiliensis ◽  
In Vitro Investigation ◽  
Bacillus Subtilis Atcc ◽  
Antimicrobial Evaluation

A series of 34 new pyrimido[2,1-c][1,2,4]triazine-3,4-diones were synthesized and fully characterized using IR, NMR, MS, and microanalytical analysis. In vitro investigation of 12 compounds of this series revealed promising antimicrobial activity of the conjugates 15a and 15f–j that were tagged with electron-withdrawing groups, with sensitivities ranging from 77% to as high as 100% of the positive control. The investigation of antimicrobial activity included Bacillus subtilis ATCC 6633, Staphylococcus aureus ATCC 6535, Pseudomonas aeruginosa ATCC 27853, and Escherichia coli ATCC 8739 (EC), and fungal strains Candida albicans ATCC 10231 and Aspergillus brasiliensis ATCC 16404.

Synthesis, PASS predication, in vitro antimicrobial evaluation and pharmacokinetic study of novel n-octyl glucopyranoside esters

2019 ◽  
Vol 485 ◽  
pp. 107812 ◽  
Author(s):  
Mohammed M. Matin ◽  
Sreebash C. Bhattacharjee ◽  
Priyanka Chakraborty ◽  
Muhammad S. Alam
Keyword(s):  
Pharmacokinetic Study ◽  
Antimicrobial Evaluation

scholarly journals Studies of Biologically Active Heterocycles: Synthesis, Characterization and Antimicrobial Activity of Some 2,5-Disubstituted-1,3,4-Oxadiazoles

1970 ◽  
Vol 6 (2) ◽  
pp. 69-75 ◽  
Author(s):  
G Nagalakshmi
Keyword(s):  
Phosphorus Oxychloride ◽  
Biologically Active ◽  
Shigella Dysenteriae ◽  
Diffusion Method ◽  
Diffusion Technique ◽  
Antimicrobial Evaluation ◽  
Bacteria And Fungi ◽  
Different Strains ◽  
Agar Well Diffusion Method

1,3,4-oxadiazoles are important because of its versatile biological actions. In the present study, several 2,5-disubstituted-1,3,4-oxadiazoles (3a-o) have been synthesized by the condensation of 4-hydroxybenzohydrazide (1) with various aromatic acids (2a-o) in presence of phosphorus oxychloride. The structures of the newly synthesized compounds have been established on the basis of elemental analysis, UV, IR and 1H NMR spectral data. The synthesized compounds were screened for their in vitro growth inhibiting activity against different strains of bacteria and fungi viz., Staphylococcus aureus, Bacillus subtilis, Bacillus megaterium, Escherichia coli, Pseudomonas aeruginosa, Shigella dysenteriae, Candida albicans, Aspergillus niger and Aspergillus flavus and the results were compared with the standard antibiotics such as chloramphenicol (50?g/ml) and Griseofulvin (50?g/ml) using agar diffusion technique. Compounds 3b, 3e, 3g, 3h, 3j, 3m and 3n exhibited strong antibacterial activity and compounds 3a, 3d, 3g, 3h and 3i showed good antifungal activity. Key words: 2,5-disubstituted-1,3,4-oxadiazoles, 4-hydroxybenzohydrazide, phosphorus oxychloride, antimicrobial evaluation, agar well diffusion method. Dhaka Univ. J. Pharm. Sci. 6(2): 69-75, 2007 (December)

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