scholarly journals Facile Synthesis, Characterization, and In Vitro Antimicrobial Screening of a New Series of 2,4,6-Trisubstituted-s-triazine Based Compounds

2015 ◽  
Vol 2015 ◽  
pp. 1-10
Author(s):  
Ravi Bhushan Singh ◽  
Nirupam Das ◽  
Md. Kamaruz Zaman
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Elemental Analysis ◽  
Broad Spectrum ◽  
Antibacterial Efficacy ◽  
Facile Synthesis ◽  
Standard Drug ◽  
E Coli

A series of new 2,4,6-trisubstituted-s-triazine was synthesized, assessed for antimicrobial activity, and characterized by FTIR, 1HNMR, 13CNMR, and elemental analysis. The tested compounds, 4d, 4g, 4h, 4k, and 4n, have shown considerable in vitro antibacterial efficacy with reference to the standard drug ciprofloxacin (MIC 3.125 μgmL−1 against B. subtilis, E. coli, and K. pneumoniae). It was observed that compounds 4d and 4h displayed equipotent antibacterial efficacy against B. subtilis (MIC 3.125 μgmL−1) and S. aureus (MIC 6.25 μgmL−1). The studies demonstrated that the para-fluorophenylpiperazine substituted s-triazine (4n) was potent and exhibited broad spectrum antibacterial activity against S. epidermidis, K. pneumoniae, and P. aeruginosa with MIC of 6.25 μgmL−1 and for E. coli, it showed an MIC of 3.125 μgmL−1 equipotent with reference to the standard drug. Among all the compounds under investigation, compound 4g also demonstrated significant antifungal activity (3.125 μgmL−1) against C. albicans.

Synthesis and Antibacterial Activity of Azetidinonyl Norfloxacin Congeners

2015 ◽  
Vol 8 (3) ◽  
pp. 2967-2971
Author(s):  
Shalabh Sharma ◽  
Kuldeep Kumar Saxena
Keyword(s):  
Antibacterial Activity ◽  
Schiff Bases ◽  
Elemental Analysis ◽  
Standard Drug ◽  
Reference Drug ◽  
E Coli ◽  
Subtilis Atcc ◽  
Structure Activity ◽  
Drug Compound

Some novel Schiff bases and azetidinone congeners of norfloxacin have been synthesized and screened for antibacterial activity. The structures of compounds 1-ethyl-6-fluoro-7-piperazinyl-4-oxo-3-(substitutedarylidinylcarboxy- hydrazido)quinolines (2-6) and 1-ethyl-6-fluoro-7-pipera-zinyl-4-oxo-3-(3′-choloro-2′-oxo-4′-substitutedaryl-3′-aze-tidinyl)-aminocarboxy quinolines (7-11) were established by spectral and elemental analysis. The compounds 2-11 were evaluated in vitro against various strains of bacteria: E. coli ATCC 25922,    B. subtilis ATCC 1633 and S. aureus ATCC 25923 to determine their antibacterial activity and feasible structure-activity relationships. The results of the study were compared with reference drug. Compound 8: 1-ethyl-6-fluoro-7-piperazinyl-4-oxo-3-(3′-choloro-2′-oxo-4′-(4′′-methoxyphenyl)-3′-azetidinyl)-aminocarboxyquinoline has displayed more potent antibacterial activity as compared to standard drug, chloramphenicol.   

scholarly journals An In Vitro Study on the Antimicrobial Properties of Essential Oil Modified Resin Composite against Oral Pathogens

Materials ◽  
2020 ◽  
Vol 13 (19) ◽  
pp. 4383
Author(s):  
Barbara Lapinska ◽  
Aleksandra Szram ◽  
Beata Zarzycka ◽  
Janina Grzegorczyk ◽  
Louis Hardan ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Resin Composite ◽  
Antimicrobial Properties ◽  
In Vitro Study ◽  
Diffusion Method ◽  
Oral Pathogens

Modifying the composition of dental restorative materials with antimicrobial agents might induce their antibacterial potential against cariogenic bacteria, e.g., S.mutans and L.acidophilus, as well as antifungal effect on C.albicans that are major oral pathogens. Essential oils (EOs) are widely known for antimicrobial activity and are successfully used in dental industry. The study aimed at evaluating antibacterial and antifungal activity of EOs and composite resin material (CR) modified with EO against oral pathogens. Ten EOs (i.e., anise, cinnamon, citronella, clove, geranium, lavender, limette, mint, rosemary thyme) were tested using agar diffusion method. Cinnamon and thyme EOs showed significantly highest antibacterial activity against S.mutans and L.acidophilus among all tested EOs. Anise and limette EOs showed no antibacterial activity against S.mutans. All tested EOs exhibited antifungal activity against C.albicans, whereas cinnamon EO showed significantly highest and limette EO significantly lowest activity. Next, 1, 2 or 5 µL of cinnamon EO was introduced into 2 g of CR and microbiologically tested. The modified CR showed higher antimicrobial activity in comparison to unmodified one. CR containing 2 µL of EO showed the best antimicrobial properties against S.mutans and C.albicans, while CR modified with 1 µL of EO showed the best antimicrobial properties against L.acidophilus.

scholarly journals 3-Amino-5-(indol-3-yl)methylene-4-oxo-2-thioxothiazolidine Derivatives as Antimicrobial Agents: Synthesis, Computational and Biological Evaluation

2020 ◽  
Vol 13 (9) ◽  
pp. 229
Author(s):  
Volodymyr Horishny ◽  
Victor Kartsev ◽  
Vasyl Matiychuk ◽  
Athina Geronikaki ◽  
Petrou Anthi ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Minimal Bactericidal Concentration ◽  
Active Compounds ◽  
Hek 293 ◽  
E Coli ◽  
Thiazolyl Blue Tetrazolium Bromide

Herein we report the design, synthesis, computational, and experimental evaluation of the antimicrobial activity of fourteen new 3-amino-5-(indol-3-yl) methylene-4-oxo-2-thioxothiazolidine derivatives. The structures were designed, and their antimicrobial activity and toxicity were predicted in silico. All synthesized compounds exhibited antibacterial activity against eight Gram-positive and Gram-negative bacteria. Their activity exceeded those of ampicillin and (for the majority of compounds) streptomycin. The most sensitive bacterium was S. aureus (American Type Culture Collection ATCC 6538), while L. monocytogenes (NCTC 7973) was the most resistant. The best antibacterial activity was observed for compound 5d (Z)-N-(5-((1H-indol-3-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)-4-hydroxybenzamide (Minimal inhibitory concentration, MIC at 37.9–113.8 μM, and Minimal bactericidal concentration MBC at 57.8–118.3 μM). Three most active compounds 5d, 5g, and 5k being evaluated against three resistant strains, Methicillin resistant Staphilococcus aureus (MRSA), P. aeruginosa, and E. coli, were more potent against MRSA than ampicillin (MIC at 248–372 μM, MBC at 372–1240 μM). At the same time, streptomycin (MIC at 43–172 μM, MBC at 86–344 μM) did not show bactericidal activity at all. The compound 5d was also more active than ampicillin towards resistant P. aeruginosa strain. Antifungal activity of all compounds exceeded those of the reference antifungal agents bifonazole (MIC at 480–640 μM, and MFC at 640–800 μM) and ketoconazole (MIC 285–475 μM and MFC 380–950 μM). The best activity was exhibited by compound 5g. The most sensitive fungal was T. viride (IAM 5061), while A. fumigatus (human isolate) was the most resistant. Low cytotoxicity against HEK-293 human embryonic kidney cell line and reasonable selectivity indices were shown for the most active compounds 5d, 5g, 5k, 7c using thiazolyl blue tetrazolium bromide MTT assay. The docking studies indicated a probable involvement of E. coli Mur B inhibition in the antibacterial action, while CYP51 inhibition is likely responsible for the antifungal activity of the tested compounds.

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, 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.

Synthesis and Antimicrobial Activity of Some New N-(1H-benzimidazol-2- yl)-2-mercaptoacetamide Derivatives

2018 ◽  
Vol 15 (2) ◽  
pp. 154-159
Author(s):  
Asaf Evrim Evren ◽  
Sinem Tekinkoca ◽  
Leyla Yurttas
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Bacterial Resistance ◽  
Fungal Infections ◽  
Antimicrobial Activities ◽  
Benzimidazole Derivatives ◽  
Standard Drug ◽  
E Coli ◽  
Pharmacological Significance ◽  
Anti Fungal

Background: Due to multi-drug, extended-drug, and pandrug resistance phenotypes, bacterial resistance to antibiotics and fungal infections are a general health issue. Particulary, increase of fungal infections due to secondary cause of human diseases have been observed. An extensive variety of benzimidazole derivatives have been characterized for their chemotherapeutic significance. Benzimidazole derivatives have received important attention because of pharmacological significance during current years, especially antimicrobial, anti-fungal, antitubercular, antioxidant, anti-Alzheimer's disease and antihypertension activities. Methods: Some N-(1H-benzimidazol-2-yl)-2-mercaptoacetamide derivatives (2a-h) were synthesised and evaluated for their antimicrobial activity. The title compounds were gained by reacting N-(1H-benzimidazol-2-yl)-2-chloroacetamide with some substituted 2-mercapto heterocyclic rings. The synthesised compounds were investigated for their antimicrobial activities against C. albicans (ATCC 24433), C. krusei (ATCC 6258), C. glabrata (ATCC90030), C. parapsilosis (ATCC 22019), E. coli (ATCC 25922), E. coli (ATCC 35218), E. feacalis (ATCC 51299), E. feacalis (ATCC 29212), S. aureus (ATCC 25923), K. pneumoniae (ATCC 700603), P. aeruginosa (ATCC 27853). Results: The compounds showed high antifungal activity when compared with standard drug ketoconazole. In addition, all compounds (MIC 100 µg/mL) showed inhibitor activity against P. aeruginosa at two fold concentration of chloramphenicol (MIC 50 µg/mL). Also, compounds 2a, 2c and 2e (MIC: 50 µg/mL) have equal effect against E. coli (ATCC 35218) and more effective than other compounds (MIC of chloramphenicol: 100 µg/mL). Conclusıon: All compounds showed notable activity. Compounds have determined to possess higher antifungal activity than antibacterial activity. Additionally, compounds 2a with 1-methyltetrazole, 2c with benzothiazole and 2e with 6-chlorobenzothiazole moieties were found as the most active compounds.

scholarly journals Synthesis and Antimicrobial Activity of 7-Hydroxy-3',4'-Methylenedioxy- and 7-Benzyloxy-3',4'-Methylenedioxy Flavanones

2017 ◽  
Vol 9 (3) ◽  
pp. 297-306 ◽  
Author(s):  
R. Ali ◽  
A. Rahim ◽  
A. Islam
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Elemental Analysis ◽  
The Other ◽  
Antifungal Activities ◽  
Fungal Strains ◽  
Antibacterial And Antifungal Activities ◽  
Other Hand ◽  
Antibacterial And Antifungal

7-Hydroxy-3',4'-methylenedioxy- and 7-benzyloxy-3',4'-methylenedioxy flavanones have been synthesized starting from 2,4-dihydroxyacetophenone. Subsequently biocidal activities of the flavanones have been investigated along with their corresponding chalcones against some bacterial and fungal strains. 2'-Hydroxy-4'-benzyloxy-3,4-methylenedioxy chalcone (5) and its corresponding flavanone (7) showed good antibacterial and antifungal activities against some selected bacterial and fungal strains. On the other hand, 2',4'-dihydroxy-3,4-methylenedioxy chalcone (4) showed no antibacterial and antifungal activities while its corresponding flavanone (6) showed a little antibacterial activity only at higher concentration but did not show antifungal activity. The synthesized chalcones and flavanones have been characterized using UV-Vis, IR and 1H NMRspectral data together with elemental analysis.

scholarly journals Synthesis of some novel 1H-indole derivatives with antibacterial activity and antifungal activity

2020 ◽  
Vol 9 (2) ◽  
pp. 961-967 ◽  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Indole Derivatives ◽  
Standard Drug ◽  
Paper Disk ◽  
Standard Medication ◽  
Tube Dilution

The present research works a series of new 1H-Indole derivatives were synthesized. The title compound was obtained by the reaction of indole with chloroacetylchloride in toluene afforded 2-chloro-1-(indoline-1-yl) ethanone which reacts with 1,4 diamine benzene in chloroform afforded 2-((4-aminophenyl)amino)-1-(1H-indol-1-yl)ethan-1-one, on further reaction with various acetophenone in presence of acetic acid in ethanol gave various final derivatives. After synthesis of compounds, the synthesized compounds were characterized by their IR, 1HNMR spectral data and elemental analysis. These derivatives were screened for their antimicrobial activity (Paper-disk-plate technique (disc diffusion method) and Tube-dilution technique (broth microdilution technique), antifungal activity of all synthesized compounds were evaluated against Aspergillus niger and Candida albicans (ATCC 10231) using Fluconazole as the standard drug using the paper plate method and antibacterial activity against both Gram-positive (Bacillus subtilis) and Gram-negative bacteria (Escherichia coli) using Ampicillin as standard medication at a concentration of 50g/ml, 100g/ml. The collected compounds were evaluated for antibacterial activity and antifungal activity. All compounds exhibit significant antimicrobial activity.

scholarly journals Invitro antibacterial activity of Cassia fistula Linn methanolic leaf extracts

2019 ◽  
Vol 8 (2) ◽  
pp. 270
Author(s):  
Bindhu R. Kamath ◽  
Sabeena Kizhedath
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Cassia Fistula ◽  
Leaf Extracts ◽  
E Coli

Background: Cassia fistula Linn is a plant which is widely grown in India and is used for medicinal purposes. The study was carried out with an objective to demonstrate the antimicrobial activity of leaves of Cassia fistula Linn. The aim of the study is to assess antibacterial and antifungal activity of methanolic leaf extract of Cassia fistula Linn against selected clinical isolates.Methods: The antimicrobial activity of methanolic extract of Cassia fistula was evaluated using agar well diffusion method and to zone of inhibition of extract was determined. Clinical isolates of Staphyloccocus aureus, MRSA, Pseudomonas aeruginosa, E. coli and Proteus were screened.Results: The methanolic extracts exhibited antibacterial activity against Staphylococcus aureus. The extract was not active against E. coli, Proteus, MRSA, Pseudomonas aeruginosa. The extract also failed to demonstrate antifungal activity against Candida albicans and Aspergillus niger.Conclusions: The global emergence of multidrug resistant bacterial strains is increasing, limiting the effectiveness of current drugs and treatment failure of infections. A novel approach to the prevention of antibiotic resistance of pathogenic species is the use of new compounds that are not based on existing synthetic antimicrobial agents.

scholarly journals A facile synthesis of 10-methoxy-4. 8-dinitro-6H-benzo [2,3-c]chromen-6-one

2004 ◽  
Vol 69 (7) ◽  
pp. 527-532 ◽  
Author(s):  
F.H. Havaldar ◽  
S. Bhise ◽  
S. Burudkar
Keyword(s):  
Antibacterial Activity ◽  
Nmr Spectroscopy ◽  
Elemental Analysis ◽  
Thionyl Chloride ◽  
Chromatographic Analysis ◽  
1H Nmr Spectroscopy ◽  
Knoevenagel Reaction ◽  
Facile Synthesis ◽  
E Coli ◽  
Carbonyl Chloride

3-Methoxy-5-nitrobenzaldehyde undergoes Knoevenagel reaction with malonic acid to give 3-methoxy-5-nitrocinnamic acid (I). Treatment of I with thionyl chloride yielded 3-chloro-5-methoxy-7-nitrobenzo[b]thiophene-2-carbonyl chloride (II) in 45 % yield. The reaction of II with 2-nitrophenol in benzene gave 2-nitrophenyl 3-chloro-5-methoxy- 7-nitrobenzo[b]thiophene-2-carboxylate (IIIa) in 65 % yield. Finally, dehydrochlorinative photocyclization of IIIa in acetone in the presence of the base triethylamine afforded 10-methoxy-4,8-dinitro-6H-benzothieno_2,3-c_chromen-6-one (IVa). Thus, a series of derivatives IVa-i were synthesized in excellent yields. The structures of the obtained products were characterized by IR and 1H-NMR spectroscopy, as well as elemental analysis. Their purity was ascertained by chromatographic analysis. All the compounds were tested for their antibacterial activity against S. aureus, E. coli, B. subtilis and S. typhosa.

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