scholarly journals Synthesis and Biological Activity Evaluation of Some Azetidinone and Thiazolidinone Derivatives of Coumarins

1970 ◽  
Vol 4 (2) ◽  
Author(s):  
BB Subudhi ◽  
PK Panda ◽  
BK Tosh ◽  
S Sahu ◽  
P Majhi
Keyword(s):  
Aromatic Aldehydes ◽  
Aluminium Chloride ◽  
Standard Drug ◽  
E Coli ◽  
Triethyl Amine ◽  
Hydroxy Coumarin ◽  
Pharmacological Potential ◽  
Different Strains ◽  
Coumarin 1

Keeping in view the pharmacological potential of azetidinones, thiazolidinones and coumarins, the title compounds containing these nuclei were synthesized. The 4-methyl -7-hydroxy coumarin (1) on treatment with hydrazine hydrate affords 2-hydrazo- 4-methyl -7-hydroxy coumarin (2). The N- (2’-imino-4’-methyl-7’-hydroxy coummarinyl)-imino substituted benzene (3) was synthesized by reaction of compound 2 with various aromatic aldehydes. Condensation of compound 3 with chloroacetyl chloride in presence of 1,4-dioxan and triethyl amine yields the 3-chloro-4- (substituted)-1-(2’-imino-4’-methyl-7’-hydroxy coumarinyl) azetidin-2-one (4a-d). Further more condensation of 3 with thioglycollic acid in presence of 1,4-dioxan and anhydrous aluminium chloride gives 2-(substituted phenyl)-3-(2’-imino-4’-methyl-7’-hydroxy coumarinyl)-1,3-thiazolidinone (4’a-d). Elemental and spectral characterization established the identity of these compounds. All the products were screened in vitro for their anti microbial activity against different strains of urinary tract pathogens. All compounds exhibited significant antimicrobial activity compared to the standard drug nitrofurantoin. Key words: Azetidinones, thiazolidinone, coumarin, nitrofurantoin, E. coli, P. auregenosa, K. pneumoniae, P. mirabilis E. faecalis, and S.aureus. Dhaka Univ. J. Pharm. Sci. Vol.4(2) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

A fraction from Escherichia coli with anti-Aspergillus properties

2005 ◽  
Vol 54 (4) ◽  
pp. 375-379 ◽  
Author(s):  
V Yadav ◽  
R Mandhan ◽  
Rajesh Dabur ◽  
A K Chhillar ◽  
J Gupta ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Protein Concentration ◽  
Exchange Chromatography ◽  
Active Molecule ◽  
Standard Drug ◽  
E Coli ◽  
Variable Activity ◽  
Sds Page ◽  
Haemolytic Assay

The products of various strains of Escherichia coli (BL21, DH5α, HB101 and XL Blue) were investigated for antimycotic properties using pathogenic isolates of Aspergillus. Co-culture experiments revealed that E. coli strains exhibited variable activity against Aspergillus fumigatus. The lysates prepared from DH5α, HB101 and XL Blue strains of E. coli showed inhibitory activity against A. fumigatus in the protein concentration range of 62.50 to 250.00 μg ml−1. The highest activity was seen in the lysate of BL21, which inhibited the growth of A. fumigatus and Aspergillus flavus completely at a concentration of 31.25 μg protein ml−1. The MIC of BL21 lysate against Aspergillus niger was found to be 62.50 μg ml−1. The in vitro toxicity of BL21 lysate was evaluated using a haemolytic assay. A BL21 lysate protein concentration of 1250.00 μg ml−1 was found to be nontoxic to human erythrocytes. The standard drug amphotericin B lysed 100 % of erythrocytes at a concentration of 37.50 μg ml−1. SDS-PAGE showed the presence of at least 15 major proteins in the lysate of BL21. Ion-exchange chromatography resolved the BL21 lysate into five fractions and fraction III was found to be endowed with anti-Aspergillus properties. The MIC of this fraction was found to be 3.90 μg ml−1. Further work on the purification of the active molecule and its characterization is in progress.

scholarly journals Synthesis and Pharmacological Evaluation of 2-(4-(3 (Substituted Phenyl) Acryloyl) Phenoxy)-N, N Diphenylacetamides

2020 ◽  
Vol 10 (5) ◽  
pp. 274-292
Author(s):  
Rohit Kumar ◽  
Sushil Kumar ◽  
Mohammad Asif Khan
Keyword(s):  
Antibacterial Activity ◽  
Schiff Bases ◽  
Biological Activities ◽  
Diffusion Method ◽  
Gram Positive ◽  
Standard Drug ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Pharmacological Evaluation

Recently a series of Schiff bases of diphenylamine derivatives have been synthesized and evaluated in vitro for their antibacterial activity against pathogenic both Gram-positive bacteria B. subtitles and Gram-negative bacteria E. coli using ciprofloxacin as standard drug at conc. of 50 μg/ml and 100 μg/ml. Literature review revels that chalcones possesses various biological activities like antimicrobial, antiviral, anti-inflammatory, anticancer and sedative etc. Therefore the present study was designed on synthesis and pharmacological evaluation of 2-(4-(3 (Substituted Phenyl) Acryloyl) Phenoxy)-N, N Diphenylacetamides. Target compound was synthesized by reaction of chloroacetylchloride with diphenylamine to afford 2-chloro-N, N-diphenylacetamide which further by reaction with substituted Chalcones and characterized following recrystallization and evaluated for anti-microbial potential through cup-diffusion method. In results, the target compounds were tested for activity against B. Subtilis, E.Coli and C. albicans. The chalcones having the lipophilic 4-chloro group (RKCT2) showed the greatest antimicrobial activity (zone of inhibition 20 & 22 mm against. B. subtilis, E. Coli, C. Albicans respectively. It suggests further researchers to go through anti-microbial evaluations against a more varieties of bacteria and fungi. Keywords: Schiff bases of diphenylamine derivatives, antibacterial activity, Gram-positive bacteria, 2-(4-(3 (Substituted Phenyl) Acryloyl) Phenoxy)-N, N Diphenylacetamides

scholarly journals SYNTHESIS, CHARACTERIZATION AND IN VITRO ANTIMICROBIAL EVALUATION OF SOME NOVEL BENZIMIDAZOLE DERIVATIVES BEARING HYDRAZONE MOIETY

2017 ◽  
Vol 10 (16) ◽  
pp. 1
Author(s):  
Jayanta Sarma ◽  
Gurvinder Singh ◽  
Mukta Gupta ◽  
Reena Gupta ◽  
Bhupinder Kapoor
Keyword(s):  
Antibacterial Properties ◽  
Antimicrobial Properties ◽  
Aromatic Aldehydes ◽  
Antibacterial Activities ◽  
Antimicrobial Activities ◽  
Benzimidazole Derivatives ◽  
E Coli ◽  
Antimicrobial Evaluation ◽  
Antibacterial Potential

Objective: The synthesis of novel benzimidazole-hydrazone derivatives has been carried out based on the previous findings that both these pharmacophores possess potent antimicrobial activities. The antibacterial properties of synthesized derivatives were screened against both Gram-positive and Gram-negative bacteria.Methods: O-phenylenediamine on condensation with substituted aromatic acids in polyphosphoric acid gave benzimidazole nucleus which on reaction with ethyl chloroacetate and hydrazine hydrate in two different steps resulted in the formation of substituted acetohydrazides. The targeted compounds 6a-l were synthesized by reaction of substituted acetohydrazides with aromatic aldehydes and screened for their antibacterial potential by cup-plate method.Results: The synthesized benzimidazole-hydrazones exhibited moderate to strong antibacterial activities against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa. The compounds 6a-6f were found to be most effective against S. aureus, E. coli, and P. aeruginosa. Among all the synthesized compounds, the zone of inhibition of 6f in highest concentration, i.e., 100 μg/ml were found to be >31 mm against all the stains of bacteria.Conclusion: The antibacterial results revealed that the synthetized derivatives have significant antimicrobial properties and further structure activity relationship studies may develop more potent and less toxic molecules.

Preparation and Standardization of Escherichia coli Nosodes Sourced from Select E. coli Strains

Homeopathy ◽  
2020 ◽  
Vol 109 (04) ◽  
pp. 207-212
Author(s):  
Renuka Munshi ◽  
Gitanjali Talele ◽  
Rajesh Shah
Keyword(s):  
Escherichia Coli ◽  
Preparation Method ◽  
Cell Extract ◽  
Molecular Testing ◽  
Chain Reaction ◽  
E Coli ◽  
Entire Cell ◽  
Polymerase Chain ◽  
Different Strains

Abstract Background The nosodes are well-known preparations in homeopathy that are sourced from organisms and diseased materials. More than 40 known nosodes have been used in homeopathic practice for over a century. Having identified the need for scientifically developed new nosodes sourced from organisms that are currently prevalent, the preparation of Escherichia coli nosodes from different strains of the bacterium is presented in this article. Materials and Methods Escherichia coli strains (E. coli ATCC 11775E, ATCC 25922, and ATCC 8739) were identified, cultured, and tested for purity, and 20 billion cells were processed following the nosode preparation method given in the Homoeopathic Pharmacopoeia of India, group N1. Serial dilution and potentization for liquid potency were done up to 30c potency. Nosodes were prepared by two methods: from cell-free extract (endotoxin) and from entire-cell extract. Result Six nosodes were developed in total. Three univalent nosodes were prepared using individual endotoxins, one from each of the three E. coli strains; those three univalent nosodes were also combined as “Trivalent nosode-I”. “Trivalent nosode-II” was prepared by mixing entire cells of the three E. coli strains. A mix of both Trivalent nosode-I and Trivalent nosode-II was labeled “EC-Polynosode”. The safety profile of the potentized nosodes was documented by the non-detectability of traces of source material (absence of contamination, live organisms, or DNA material) through a culture test, sterility test, and molecular testing (polymerase chain reaction). Conclusion Different variants of E. coli nosodes were systematically and scientifically prepared and standardized using the cultures. Homeopathic pathogenetic trials, in-vitro efficacy studies, and clinical evaluation of E. coli nosodes (single, trivalent, or polyvalent nosodes) will be required in future.

Synthesis of some novel 6′-(4-chlorophenyl)-3,4′-bipyridine-3′-carbonitriles: assessment of their antimicrobial and cytotoxic activity

2015 ◽  
Vol 70 (11) ◽  
pp. 783-795 ◽  
Author(s):  
Essam M. Hussein ◽  
Hossa F. Al-Shareef ◽  
Amany H. Aboellil ◽  
Heba A. Elhady
Keyword(s):  
Cytotoxic Activity ◽  
Antimicrobial Agents ◽  
Trichoderma Viride ◽  
Human Tumor ◽  
Cancer Cell Line ◽  
Aromatic Aldehydes ◽  
Standard Drug ◽  
Gram Positive Bacteria ◽  
Tosyl Chloride

AbstractA series of novel substituted 6′-(4-chlorophenyl)-3,4′-bipyridine-3′-carbonitriles with incorporated pyrazole and/or triazole moieties have been synthesized using 2-(6′-(4-chlorophenyl)-3′-cyano-3,4′-bipyridin-2′-yloxy)acetohydrazide (3) as starting material. Also, the key intermediate 3 reacted with aromatic aldehydes and tosyl chloride to give the corresponding Schiff bases and tosyl hydrazide derivatives, respectively. The antimicrobial of these newly synthesized compounds was evaluated against Bacillus subtilis as Gram-positive bacteria and Trichoderma viride as a fungus; some of these compounds such as 5, 6, 7, 8, 10, 12, and 14 showed excellent activities as antimicrobial agents. Moreover, the cytotoxic activity of the most active compounds was assessed in vitro against human tumor liver cancer cell line (HEPG2); compounds 8, 10, 13a, and 14 showed potent activities relative to Doxorubicin which was used as a reference standard drug in this study.

scholarly journals Thiazolo-Pyrimidine Analogues: Synthesis, Characterization and Docking Studies Guided Antimicrobial Activities

2020 ◽  
Vol 11 (2) ◽  
pp. 9443-9455
Keyword(s):  
Aromatic Aldehydes ◽  
Dna Gyrase ◽  
Docking Study ◽  
Antimicrobial Activities ◽  
Docking Studies ◽  
One Pot ◽  
Standard Drug ◽  
Toluene Sulfonic Acid ◽  
Pyrimidine Analogues

In the current study, bicyclic 1-(7-methyl-3,5-diphenyl-5H-thiazolo(3,2-α)pyrimidine-6-yl)ethanone (4a-l) derivatives have been designed and conveniently synthesized by one-pot three-component method via cyclocondensation of substituted 4-phenylthiazole-2-amine (1a-c), acetylacetone (2) and various aromatic aldehydes (3a-d) in the presence of p-toluene sulfonic acid (PTSA) under acetonitrile solvent medium. The synthesized compounds (4a-l) have been characterized by spectral analysis and subjected to docking study against protein DNA gyrase (PDB Code: 1KZN), and also, the compounds were screened for their in vitro antimicrobial activities. The bioassay of the synthesized compounds envisioned that the compound 4k emerged as a broad-spectrum antibacterial agent, and 4l emerged as a good antifungal agent compared to standard drug.

scholarly journals Novel Synthesis and Antimicrobial Activities of Thiazino-Oxazine Derivatives

2018 ◽  
Vol 10 (4) ◽  
Author(s):  
Dr.Pravina B. Piste
Keyword(s):  
Spectral Analysis ◽  
Heterocyclic Compounds ◽  
Antibacterial Activities ◽  
Antimicrobial Activities ◽  
Plate Method ◽  
Standard Drug ◽  
Gram Negative ◽  
E Coli ◽  
Novel Synthesis

In the designing and synthesis of new heterocyclic compounds, containing two different pharmacophores, we have carried out new series of 3-(4-chlorophenyl)-4-methylidene-4,8-dihydro-2H,5H-1,3-thiazino[5,4-e]-1,3-oxazine-2,5,7(3H)-trione derivatives (5a-5k) in good yields from the cyclization of 5-[(1E)-N- (4-chlorophenyl) ethanimidoyl] -4-hydroxy- 2H-1,3- thiazine-2,6(3H)-dione derivatives (4a-4k) with triphosgene. All the synthesized compounds (5a-5k) were confirmed by spectral analysis. The synthesized compounds (5a-5k) were screened in vitro for their antibacterial activities against S. subtilis (gram positive) and E. coli. (gram negative) while antifungal activity against C. albicans by cup plate method. Some of the products of series were found to have quite good activities as compared to the standard drug streptomycin and flucanozole.

scholarly journals Synthesis, DFT Analysis, and Evaluation of Antibacterial and Antioxidant Activities of Sulfathiazole Derivatives Combined with In Silico Molecular Docking and ADMET Predictions

2021 ◽  
Vol 2021 ◽  
pp. 1-14
Author(s):  
Yoseph Samuel ◽  
Ankita Garg ◽  
Endale Mulugeta
Keyword(s):  
Molecular Docking ◽  
In Silico ◽  
Radical Scavenging ◽  
Basis Set ◽  
Diffusion Method ◽  
Standard Drug ◽  
Gram Negative ◽  
E Coli ◽  
In Silico Molecular Docking

Synthetic modifications of sulfathiazole derivatives become an interesting approach to enhance their biological properties in line with their applications. As a result, sulfathiazole derivatives become a good candidate and potential class of organic compounds to play an important role towards medicinal chemistry. In present study, one thiazole derivative and two new sulfathiazole derivatives are synthesized with 94% and 72–81% yields, respectively. Furthermore, the synthesized compounds were evaluated for their in vitro antibacterial activity against two Gram-negative (E. coli and P. aeruginosa) and two Gram-positive bacterial strains (S. pyogenes and S. aureus) by disk diffusion method. Among synthesized compounds, compound 11a showed potent inhibitory activity against Gram-negative, E. coli with 11.6 ± 0.283 mm zone of inhibition compared to standard drug sulfamethoxazole (15.7 ± 0.707 mm) at 50 mg/mL. The radical scavenging activities of these compounds were evaluated using DPPH radical assay, and compound 11a showed the strongest activity with IC50 values of 1.655 μg/mL. The synthesized compounds were evaluated for their in silico molecular docking analysis using S. aureus gyrase (PDB ID: 2XCT) and human myeloperoxidase (PDB ID: 1DNU) and were found to have minimum binding energy ranging from −7.8 to −10.0 kcal/mol with 2XCT and −7.5 to −9.7 with 1DNU. Compound 11a showed very good binding score −9.7 kcal/mol with both of the proteins and had promising alignment with in vitro results. Compound 11b also showed high binding scores with both proteins. Drug likeness and ADMET of synthesized compounds were predicted. The DFT analysis of synthesized compounds was performed using Gaussian 09 and visualized through Gauss view 6.0. The structural coordinates of the lead compounds were optimized using B3LYP/6–31 G (d,p) level basis set without any symmetrical constraints. Studies revealed that all the synthesized compounds might be candidates for further antibacterial and antioxidant studies.

scholarly journals Syntheses of 2-(6’-Fluorobenzothiazol-2’-ylamino)-4, 6-(disubstituted thiouriedo)-1,3-pyrimidine Derivatives as Antimicrobial Agents

2011 ◽  
Vol 8 (1) ◽  
pp. 240-244 ◽  
Author(s):  
Anoop K. Pathak ◽  
Viney Chawla ◽  
Shailendra K. Saraf
Keyword(s):  
Antibacterial Activity ◽  
Antimicrobial Agents ◽  
Inhibiting Activity ◽  
Pyrimidine Derivatives ◽  
E Coli ◽  
Diffusion Technique ◽  
Nucleophilic Reagents ◽  
Different Strains ◽  
Growth Inhibiting

A new series of 1,3-pyrimidine derivatives (3a-f) have been synthesized by reacting 2,4,6-Trichloropyrimidine with nucleophilic reagents 2-amino-6-fluorobenzothiazole (1) in the presence of acetone. The (4,6- dichloro-pyrimidin-2-yl)-amine (2) so produced was then reacted to two moles of phenylthiourea derivatives to yield title compounds (3a-f). The structural assessment of the compounds (3a-f) was made on the basis of spectral data. The synthesized compounds were screened for theirin vitrogrowth inhibiting activity against different strains of bacteriaviz.,B. subtilis, E. coli, P. aeruginosaandS. aureususing agar diffusion technique. Compounds3cand3fexhibited highest antibacterial activity.

scholarly journals Synthesis and antibacterial activity of some 3-(5-aryl-4H-pyrazol-3-yl) anthracen-10(9H)-ones

2014 ◽  
Vol 2 (03) ◽  
pp. 12-17
Author(s):  
Harish Kumar ◽  
Sandeep Jain ◽  
Neelam Jain
Keyword(s):  
Escherichia Coli ◽  
Antibacterial Activity ◽  
Acetyl Chloride ◽  
Aromatic Aldehydes ◽  
Catalytic Amount ◽  
Standard Drug ◽  
Gram Negative ◽  
In Vitro Antibacterial Activity ◽  
And Staphylococcus Aureus

A series of 3-(5-aryl-4H-pyrazol-3-yl)anthracen-10(9H)-ones were synthesized from anthracen-10(9H)-one (1) and studied for their in vitro antibacterial activity. Anthracen- 10(9H)-one after Friedel crafts acetylation with acetyl chloride yielded 3-acetylanthracen- 10(9H)-one (2) which on further reaction with substituted aromatic aldehydes in the presence of catalytic amount of sodium hydroxide in water and ethanol furnished the corresponding 3-(3-arylacryloyl)anthracen-10(9H)-ones (3a-g) as intermediate compounds, which on further reaction with hydrazine hydrate in absolute ethanol formed the title compounds 3-(5-aryl-4H-pyrazol-3-yl)anthracen-10(9H)-ones (4a-g). These compounds were characterized by elemental analysis, IR, Mass and 1H-NMR spectral data. All the compounds were evaluated for their in vitro antibacterial activity against two gram positive strains (Bacillus subtilis and Staphylococcus aureus) and two gram negative strains (Escherichia coli and Pseudomonas aeruginosa) taking ciprofloxacin as a standard drug. Some of the compounds showed significant antibacterial activity.

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