scholarly journals Eco-Friendly, Green Approach for Synthesis of Bio-Active Novel 3-Aminoindazole Derivatives

2021 ◽  
Author(s):  
Chandrashekhar Devkate ◽  
Satish Kola ◽  
Mohammad Idrees ◽  
Naqui J. Siddiqui ◽  
Roshan D. Nasare
Keyword(s):  
Antimicrobial Activity ◽  
Efficient Method ◽  
Ultrasound Irradiation ◽  
Spectral Studies ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Gram Negative ◽  
Green Approach ◽  
Pathogenic Microbe

In present chapter we have reported green and highly efficient method for synthesize novel series of substituted -1H-indazol-3-amine derivative (3a-h) by cyclocondensation reaction of substituted benzonitrile (1a-h) and substituted Hydrazine (2a-h) using ceric (IV) ammonium nitrate (CAN) as a catalyst, EtOH-H2O as a ecofriendly media and reaction was carried out under ultrasound irradiation green method. The structures of newly synthesized indazole derivative (3a-h) were corroborated through spectral investigation such as elemental analysis and spectral studies like IR, C13 NMR, Mass spectra and 1H NMR. The compounds were assessed for their in-vitro antimicrobial activity with pathogenic microbe comprising Gram positive bacterial strains, S. aureus and Gram negative strains E.coli, P.vulgaris, and S. typhi at different concentration. The consequence of bioassay is compared with standard drug Chloramphenicol.

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.

scholarly journals Antimicrobial Activity and DNA/BSA Binding Affinity of Polynuclear Silver(I) Complexes with 1,2-Bis(4-pyridyl)ethane/ethene as Bridging Ligands

2020 ◽  
Vol 2020 ◽  
pp. 1-12
Author(s):  
Sonja Ž. Đurić ◽  
Sandra Vojnovic ◽  
Tina P. Andrejević ◽  
Nevena Lj Stevanović ◽  
Nada D. Savić ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Therapeutic Potential ◽  
Fibroblast Cell ◽  
Bacterial Strains ◽  
Human Lung Fibroblast ◽  
Gram Negative ◽  
Minimal Inhibitory Concentrations ◽  
Lung Fibroblast Cell Line ◽  
Bacteria And Fungi

1,2-Bis(4-pyridyl)ethane (bpa) and 1,2-bis(4-pyridyl)ethene (bpe) were used for the synthesis of polynuclear silver(I) complexes, {[Ag(bpa)]NO3}n (1), {[Ag(bpa)2]CF3SO3.H2O}n (2) and {[Ag(bpe)]CF3SO3}n (3). In complexes 1–3, the corresponding nitrogen-containing heterocycle acts as a bridging ligand between two Ag(I) ions. In vitro antimicrobial activity of these complexes, along with the ligands used for their synthesis, was evaluated against the broad panel of Gram-positive and Gram-negative bacteria and fungi. The silver(I) complexes 1–3 showed selectivity towards Candida spp. and Gram-negative Escherichia coli in comparison to the other investigated bacterial strains, effectively inhibiting the growth of four different Candida species with minimal inhibitory concentrations (MICs) between 2.5 and 25 μg/mL and the growth of E. coli, with MIC value being 12.5 μg/mL. Importantly, complex 2 significantly reduced C. albicans filamentation, an essential process for its pathogenesis. Antiproliferative effect on the normal human lung fibroblast cell line MRC-5 was also evaluated with the aim of determining the therapeutic potential of the complexes 1–3. The interactions of these complexes with calf thymus DNA (ctDNA) and bovine serum albumin (BSA) were studied to evaluate their binding activities towards these biomolecules for possible insights on their mode of action.

scholarly journals In Vitro Bactericidal Activity of Human β-Defensin 3 against Multidrug-Resistant Nosocomial Strains

2006 ◽  
Vol 50 (2) ◽  
pp. 806-809 ◽  
Author(s):  
Giuseppantonio Maisetta ◽  
Giovanna Batoni ◽  
Semih Esin ◽  
Walter Florio ◽  
Daria Bottai ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Bactericidal Activity ◽  
Stenotrophomonas Maltophilia ◽  
Bactericidal Effect ◽  
Multidrug Resistant ◽  
Bacterial Strains ◽  
Gram Negative

ABSTRACT The antimicrobial activity of human β-defensin 3 (hBD-3) against multidrug-resistant clinical isolates of Staphylococcus aureus, Enterococcus faecium, Pseudomonas aeruginosa, Stenotrophomonas maltophilia, and Acinetobacter baumannii was evaluated. A fast bactericidal effect (within 20 min) against all bacterial strains tested was observed. The presence of 20% human serum abolished the bactericidal activity of hBD-3 against gram-negative strains and reduced the activity of the peptide against gram-positive strains.

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.

scholarly journals Design, Synthesis, and Evaluation of Novel 3-, 4-substituted, and 3,4-di Substituted Quinazoline Derivatives as Antimicrobial Agents

2020 ◽  
Vol 71 (2) ◽  
pp. 422-435
Author(s):  
Farag A. El-Essawy ◽  
Abdulrahman I. Alharthi ◽  
Mshari A. Alotaibi ◽  
Nancy E. Wahba ◽  
Nader M. Boshta
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Design Synthesis ◽  
Gram Negative ◽  
Spectroscopic Analyses ◽  
Quinazoline Derivatives

A novel series of 3-, 4-substituted, and 3,4-di substituted quinazoline derivatives were prepared via various cyclized regents and most of the newly prepared compounds evaluated for their antimicrobial activities in vitro against Gram-positive, Gram-negative bacterial strains and fungi strains. The structures of the quinazoline derivatives have been confirmed using spectroscopic analyses (IR, NMR, and EI-MS). Some of the synthesized derivatives displayed a moderate antimicrobial activity in comparison with reference drugs, for example compounds 13d, 15a, 17b, 18b, 18d, 25, and 29a-c. Among the synthesized compounds, the pyrimidoqunazoline derivative 6c elicited the highest activity.

In vitro Antimicrobial Activity of Liposomes Containing Ciprofloxacin,Meropenem and Gentamicin Against Gram-Negative Clinical Bacterial Strains

2007 ◽  
Vol 4 (4) ◽  
pp. 297-304 ◽  
Author(s):  
Jerzy Gubernator ◽  
Zuzanna Drulis-Kawa ◽  
Agata Dorotkiewicz-Jach ◽  
Wlodzimierz Doroszkiewicz ◽  
Arkadiusz Kozubek
Keyword(s):  
Antimicrobial Activity ◽  
Bacterial Strains ◽  
Gram Negative ◽  
In Vitro Antimicrobial Activity

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 In vitro antibacterial activity of essential oils from Lamiaceae species

2016 ◽  
Vol 5 (4) ◽  
pp. 141-144
Author(s):  
Vinod Kumar ◽  
◽  
C. S. Mathela ◽  
Amit Panwar ◽  
◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Essential Oils ◽  
Broad Spectrum ◽  
Antibacterial Effect ◽  
Gram Negative Bacteria ◽  
Bacterial Strains ◽  
Gram Negative ◽  
In Vitro Antibacterial Activity

Essential oils from Calamintha umbrosa and Nepeta species viz. N. leucophylla; N. hindostana; N. ciliaris and N. clarkei (family Lamiaceae), was tested against six bacterial strains. To evaluate the correlation between the antimicrobial activity and the essential oils, PCA and HCA analysis was done. PCA and HCA analysis of the antibacterial activity revealed that essential oils of Nepeta species had a strong and broad spectrum antibacterial effect against bacterial strains of P. aeruginosa and S. scandidus. The N. leucophylla oil showed higher activity against Gram-negative bacteria P. aeruginosa (10.5 mm, MIC 10 µL/mL) and K. pneumonia (9.1 mm, MIC 45 µL/mL) among all Nepeta oils which may be due to presence of active antimicrobial iridoids compounds.

scholarly journals 169 Susceptibility of several species of gram-negative and gram-positive bacteria to organic acids and their derivatives

2019 ◽  
Vol 97 (Supplement_2) ◽  
pp. 96-97
Author(s):  
Lauren Kovanda ◽  
Xunde Li ◽  
Wen Zhang ◽  
Xiaohong Wei ◽  
Jia Luo ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Organic Acids ◽  
Formic Acid ◽  
Butyric Acid ◽  
Sodium Formate ◽  
Valeric Acid ◽  
Bacterial Strains ◽  
Gram Positive ◽  
Gram Negative

Abstract The objective of this experiment was to determine the in vitro antimicrobial activity of several organic acids and their derivatives against gram-positive (G+) and gram-negative (G-) bacteria. Monopropionin, monovalerin, monolaurin, and sodium formate were tested at 10 to 12 concentrations from 0.001 to 2.50 mg/L; monobutyrin was tested at 16 concentrations from 0.001 to 5.00 mg/L; butyric acid and valeric acid were tested at 8 concentrations from 0.001 to 0.35 mg/L; while formic acid was tested at 8 concentrations from 0.001 to 1.00 mg/L. The tested bacteria included G- bacteria (Escherichia coli, Salmonella typhimurium, and Campylobacter jejuni) and G+ bacteria (Enterococcus faecalis, Clostridia perfringens, Streptococcus pneumonia, and Streptococcus suis). Antimicrobial activity of tested compounds was expressed as minimum inhibitory concentration (MIC) that prevented growth of tested bacteria in treated culture broth. Butyric acid, valeric acid, and formic acid at highest tested concentrations inhibited the growth of all bacterial strains. The MICs of the three acids varied among bacterial strains with lowest MIC of 0.05–0.10 mg/L on two strains of Campylobacter. Sodium formate at highest tested concentrations did not inhibit the growth of E. coli, S. typhimurium, and E. faecalis but the compound inhibited the growth of other tested bacteria with MIC values from 0.20 to 1.88 mg/L. The MIC values of monovalerin, monolaurin, and monobutyrin ranged between 0.001 and 1.50 mg/L on all bacterial strains with the exception that monobutyrin did not inhibit C. jejuni (ATCC 33560) growth at the highest concentration tested (5.0 mg/L). Monopropionin at tested concentrations did not inhibit the growth of all tested bacteria with the exception of 1.13 mg/L as MIC on C. perfringens (ATCC 12915). The MIC tests indicate that all organic acids and their derivatives, except monopropionin, tested in this experiment exhibited strong antimicrobial effects in vitro against tested bacterial strains.

Synthesis, Characterization and Antimicrobial Activity of Bis-Acetylferrocene Schiff Base

2011 ◽  
Vol 396-398 ◽  
pp. 1875-1878 ◽  
Author(s):  
Yu Ting Liu ◽  
Hai Long Guo ◽  
Da Wei Yin
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Bacillus Subtilis ◽  
Salmonella Typhi ◽  
Bacterial Strains ◽  
Gram Negative ◽  
And Staphylococcus Aureus

Three bis-acetylferrocene schiff bases have been synthesized and characterized by IR, 1H NMR, and elemental analysis, the results conformed well with expected structures. The synthesized compounds were screened in vitro for their antimicrobial activity against three Gram-negative (Escherichia coli, Pseudomonas aeruginosa, and Salmonella typhi) and two Gram-positive (Bacillus subtilis and Staphylococcus aureus) bacterial strains. The results showed that these compounds are show excellent antimicrobia activities against Escherichia coli, Pseudomonas aeruginosa, Salmonella typhi ,Bacillus subtilis,Staphylococcus aureus.

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