scholarly journals Indole-3-carbaldehyde Semicarbazone Derivatives: Synthesis, Characterization, and Antibacterial Activities

2020 ◽  
Vol 2020 ◽  
pp. 1-9 ◽  
Author(s):  
Fernando Carrasco ◽  
Wilfredo Hernández ◽  
Oscar Chupayo ◽  
Celedonio M. Álvarez ◽  
Sandra Oramas-Royo ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Bacillus Subtilis ◽  
Antibacterial Activities ◽  
Isomeric Form ◽  
Bacterial Strains ◽  
H Nmr ◽  
Nmr Techniques ◽  
Ft Ir ◽  
Liquid Acetone

Four indole-3-carbaldehyde semicarbazone derivatives, 2-((5-bromo-1H-indol-3-yl)methylene)hydrazinecarboxamide (1), 2-((5-chloro-1H-indol-3-yl)methylene)hydrazinecarboxamide (2), 2-((5-methoxy-1H-indol-3-yl)methylene)hydrazinecarboxamide (3), and 2-((4-nitro-1H-indol-3-yl)methylene)hydrazinecarboxamide (4) were synthesized and characterized by ESI-MS and spectroscopic (FT-IR, 1H NMR, and 13C NMR) techniques. The two-dimensional NMR (in acetone-d6) spectral data revealed that the molecules 1 and 2 in solution are in the cisE isomeric form. This evidence is supported by DFT calculations at the B3LYP/6-311++G(d,p) level of theory where it was shown that the corresponding most stable conformers of the synthesized compounds have a cisE geometrical configuration, in both the gas and liquid (acetone and DMSO) phases. The in vitro antibacterial activity of compounds 1–4 was determined against Gram-positive (Staphylococcus aureus and Bacillus subtilis) and Gram-negative (Pseudomonas aeruginosa and Escherichia coli) bacteria. Among all the tested semicarbazones, 1 and 2 exhibited similar inhibitory activities against Staphylococcus aureus (MIC = 100 and 150 μg/mL, respectively) and Bacillus subtilis (MIC = 100 and 150 μg/mL, respectively). On the other hand, 3 and 4 were relatively less active against the tested bacterial strains compared with 1, 2, and tetracycline.

Characterization of Antibacterial Proanthocyanidins of Dalbergia monetaria, an Amazonian Medicinal Plant, by UHPLC-HRMS/MS

Planta Medica ◽  
2020 ◽  
Vol 86 (12) ◽  
pp. 858-866
Author(s):  
Patricia Homobono Brito de Moura ◽  
Amaryllis Almeida de Sousa ◽  
Andrea Porzel ◽  
Ludger A. Wessjohann ◽  
Ivana Correa Ramos Leal ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Pathogenic Bacteria ◽  
Neutral Loss ◽  
Antibacterial Activities ◽  
Quinone Methide ◽  
In Vitro Assays ◽  
Fragmentation Pattern ◽  
Bacterial Strains ◽  
Tract Infections

Abstract Dalbergia monetaria is an Amazonian plant whose bark is widely used to treat urinary tract infections. This paper describes a bio-guided study of ethanolic extracts from the bark and leaves of D. monetaria, in a search for metabolites active against human pathogenic bacteria. In vitro assays were performed against 10 bacterial strains, highlighting methicillin-sensitive Staphylococcus aureus and methicillin-resistant Staphylococcus aureus and Pseudomonas aeruginosa. Fractioning of the extracts was performed using instrumental and classical techniques, and samples were characterized by UHPLC-HRMS/MS. Ethyl acetate fractions from bark and leaves showed similar antibacterial activities. EAFB is enriched in isoflavone C-glucosides and EAFL enriched in proanthocyanidins. Subfractions from EAFL presented higher activity and showed a complex profile of proanthocyanidins constructed by (epi)-cassiaflavan and (epi)-catechin units, including dimers, trimers and tetramers. The fragmentation pattern emphasized the neutral loss of cassiaflavan units by quinone-methide fission. Fraction SL7-6, constituted by (ent)-cassiaflavan-(ent)-cassiaflavan-(epi)-catechin isomers, showed the lowest MIC against the S. aureus and P. aeruginosa with values corresponding to 64 and 32 µg/mL, respectively. Cassiaflavan-proanthocyanidins have not been found previously in another botanical genus, except in Cassia, and the traditional medicinal use of D. monetaria might be related to the antibacterial activity of proanthocyanidins characterized in the species.

Synthesis and Antibacterial Evaluation of Thiouracil Derivatives Contain-ing 1,2,4-Triazolo[1,5-a]Pyrimidine

2020 ◽  
Vol 17 ◽  
Author(s):  
Penglei Cui ◽  
Di Zhang ◽  
Xiumin Guo ◽  
Shujing Ji ◽  
Qingmei Jiang
Keyword(s):  
Staphylococcus Aureus ◽  
Bacillus Subtilis ◽  
Inhibitory Activity ◽  
Bacillus Amyloliquefaciens ◽  
Antibacterial Activities ◽  
Inhibitory Activities ◽  
New Compounds ◽  
Thiouracil Derivatives ◽  
Antibacterial Evaluation

: A series of new thiouracil compounds containing 1,2,4-triazolo[1,5-a]pyrimidine were designed and synthesized. The in vitro antibacterial activities of the new compounds against Bacillus amyloliquefaciens, Staphylococcus aureus and Bacillus subtilis were tested. The results showed that some of the new compounds had strong inhibitory activities against the tested bacteria. At the concentration of 50 μg/mL, the compound 12d had broad and the highest inhibitory activity with the 100% inhibition against the three tested strains, the same as norfloxacin which was used as the control.

scholarly journals Benzenesulfonylation of Methyl α-D-Glucopyranoside: Synthesis, Characterization and Antibacterial Screening

2016 ◽  
Vol 64 ◽  
pp. 95-105 ◽  
Author(s):  
Sarkar M.A. Kawsar ◽  
Samia S.B.S. Nishat ◽  
Mohammad A. Manchur ◽  
Yasuhiro Ozeki
Keyword(s):  
Evaluation Studies ◽  
Antibacterial Activities ◽  
Bacterial Strains ◽  
H Nmr ◽  
Antibacterial Screening ◽  
Direct Acylation ◽  
Derivatives Of ◽  
Molecular Framework ◽  
Acyl Derivatives

A novel series of benzenesulfonyl derivatives of methyl α-D-glucopyranoside (1) were synthesized by reacting benzenesulfonyl chloride in pyridine followed by direct acylation method to yield 6-O-benzenesulfonyl derivative (2). In order to obtain newer products for antibacterial evaluation studies, the 6-O-benzenesulfonyl derivative was further transformed to a series of 2,3,4-tri-O-acyl derivatives (3-11) containing a wide variety of functionalities in a single molecular framework. All the synthesized compounds have been confirmed by IR,1H NMR and elemental analysis. These newly synthesized compounds were screened forin vitroantibacterial activity against some human pathogenic bacterial strains. The study revealed that the acylated products exhibit moderate to good antibacterial activities. It was interesting to observe that the selected compounds were more sensitive against Gram-Ve bacteria than that of the Gram-+Ve 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.

scholarly journals Synthesis and Antimicrobial Activity of Coumarinyl Schiff Base Derivatives

2014 ◽  
Vol 30 ◽  
pp. 193-201 ◽  
Author(s):  
Arun Mishra ◽  
Jaynt Rathod ◽  
Dipti Namera ◽  
Shailesh Thakrar ◽  
Anamik Shah
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Gram Negative ◽  
H Nmr ◽  
Schiff Base Derivatives ◽  
Test Organisms ◽  
Ft Ir ◽  
C Nmr

We have reported some novel N’-[(1)-ethylidene]-2-(6-methyl-2-oxo-2H-chromen-4-yl) acetohydrazide synthesized by conventional method. The reaction of 2-(6-methyl-2-oxo-2H-chromen-4-yl)acetohydrazide with substituted benzaldehyde in methanol as a solvent yielded a series of (7a-l). The structures of all synthesized compounds are well characterized by Mass, FT-IR, 1H NMR, 13C NMR and elemental analysis. Moreover, all synthesized compounds were screened for In Vitro antimicrobial activity against the gram positive (Staphylococcus aureus, Bacilluas subtilis) and gram negative (Escherichia coli, P. aeruginosa, K. pneunonae, Enterobacter) bacterial strain. In which some the compounds show potential inhibition against the test organisms.

scholarly journals Synthesis, Characterization, and Antibacterial Activities of Novel Sulfonamides Derived through Condensation of Amino Group Containing Drugs, Amino Acids, and Their Analogs

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
Muhammad Abdul Qadir ◽  
Mahmood Ahmed ◽  
Muhammad Iqbal
Keyword(s):  
Amino Acids ◽  
Spectral Analysis ◽  
New Products ◽  
Antibacterial Activities ◽  
Amino Group ◽  
Bacterial Strains ◽  
Zone Of Inhibition ◽  
E Coli ◽  
Ft Ir

Novel sulfonamides were developed and structures of the new products were confirmed by elemental and spectral analysis (FT-IR, ESI-MS,1HNMR, and13CNMR). In vitro, developed compounds were screened for their antibacterial activities against medically important gram (+) and gram (−) bacterial strains, namely,S. aureus,B. subtilis,E. coli, andK. pneumoniae. The antibacterial activities have been determined by measuring MIC values (μg/mL) and zone of inhibitions (mm). Among the tested compounds, it was found that compounds 5a and 9a have most potent activity againstE. coliwith zone of inhibition:31±0.12 mm (MIC: 7.81 μg/mL) and30±0.12 mm (MIC: 7.81 μg/mL), respectively, nearly as active as ciprofloxacin (zone of inhibition:32±0.12 mm). In contrast, all the compounds were totally inactive against the gram (+)B. subtilis.

scholarly journals Design, Synthesis and Biological Evaluation of Novel Benzothiazole Based [1,2,4]Triazolo[4,3-c]quinazoline Derivatives

2020 ◽  
Vol 32 (3) ◽  
pp. 580-586
Author(s):  
Ranjit V. Gadhave ◽  
Bhanudas S. Kuchekar
Keyword(s):  
Biological Evaluation ◽  
Bacterial Strains ◽  
Active Compounds ◽  
Design Synthesis ◽  
Structural Modifications ◽  
E Coli ◽  
Chemical Structures ◽  
Ft Ir ◽  
Antioxidant Agent

A new series of N-(benzo[d]thiazol-2-yl)-[1,2,4]triazolo[4,3-c]quinazoline-5-carboxamide derivatives were synthesized by condensation of [1,2,4]triazolo[4,3-c]quinazoline-5-carboxylate derivatives with substituted benzothiazoles. The chemical structures of the synthesized compounds were confirmed by FT-IR, MS and 1H NMR spectra. Designed triazoloquinazoline derivatives were docked with oxido-reductase enzyme (PDB Code 4h1j) and DNA gyrase enzyme (PDB Code 3g75). Based on high binding affinity score, the best compound were selected for synthesis and subjected to in vitro antioxidant and antibacterial activity. Compounds 7a and 7d were found to be most active compounds as antioxidant agent among this series when compared with ascorbic acid. Compounds 7a, 7d and 7f were found to be most active compounds as an antibacterial agents among this series when compared with ciprofloxacin against bacterial strains such as S. aureus (ATCC 25923), E. coli (ATCC 25922) and P. aeruginosa (ATCC 27853). Study revealed that the most active compounds after structural modifications can be exploited as lead molecules for other pharmacological activities such as anti-inflammatory, anticancer and antidepressant activities.

scholarly journals In VitroActivities of Daptomycin-, Vancomycin-, and Teicoplanin-Loaded Polymethylmethacrylate against Methicillin-Susceptible, Methicillin-Resistant, and Vancomycin-Intermediate Strains of Staphylococcus aureus

2011 ◽  
Vol 55 (12) ◽  
pp. 5480-5484 ◽  
Author(s):  
Yuhan Chang ◽  
Wen-Chien Chen ◽  
Pang-Hsin Hsieh ◽  
Dave W. Chen ◽  
Mel S. Lee ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
High Performance ◽  
Low Dose ◽  
Antibacterial Activities ◽  
High Dose ◽  
Bone Cements ◽  
Antibacterial Effects ◽  
Methicillin Resistant ◽  
Content Type

ABSTRACTThe objective of this study was to evaluate the antibacterial effects of polymethylmethacrylate (PMMA) bone cements loaded with daptomycin, vancomycin, and teicoplanin against methicillin-susceptibleStaphylococcus aureus(MSSA), methicillin-resistantStaphylococcus aureus(MRSA), and vancomycin-intermediateStaphylococcus aureus(VISA) strains. Standardized cement specimens made from 40 g PMMA loaded with 1 g (low-dose), 4 g (middle-dose) or 8 g (high-dose) antibiotics were tested for elution characteristics and antibacterial activities. The patterns of release of antibiotics from the cement specimens were evaluated usingin vitrobroth elution assay with high-performance liquid chromatography. The activities of broth elution fluid against differentStaphylococcus aureusstrains (MSSA, MRSA, and VISA) were then determined. The antibacterial activities of all the tested antibiotics were maintained after being mixed with PMMA. The cements loaded with higher dosages of antibiotics showed longer elution periods. Regardless of the antibiotic loading dose, the teicoplanin-loaded cements showed better elution efficacy and provided longer inhibitory periods against MSSA, MRSA, and VISA than cements loaded with the same dose of vancomycin or daptomycin. Regarding the choice of antibiotics for cement loading in the treatment ofStaphylococcus aureusinfection, teicoplanin was superior in terms of antibacterial effects.

scholarly journals Synthesis and Antibacterial Activity of New Spiro[thiadiazoline-(pyrazolo[3,4-d]pyrimidine)] Derivatives

2015 ◽  
Vol 2015 ◽  
pp. 1-6 ◽  
Author(s):  
Mohammed El Fal ◽  
Youssef Ramli ◽  
Abdelfettah Zerzouf ◽  
Ahmed Talbaoui ◽  
Youssef Bakri ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Spectroscopic Data ◽  
Heterocyclic Compounds ◽  
Dipolar Cycloaddition ◽  
Bacterial Strains ◽  
Pyrimidine Derivatives ◽  
H Nmr ◽  
Biological Interest ◽  
Mic Value

New heterocyclic compounds spiroderivatives of allopurinol of biological interest were prepared from allopurinol via thionation and 1,3-dipolar cycloaddition and were produced in high to excellent yields. These compounds were characterized on the basis of spectral and spectroscopic data (1H NMR,13C, IR, and MS). The antibacterial activity of the synthesized products was studied using bacterial strains:Staphylococcus aureus,Enterococcus faecalis,Escherichia coli, andPseudomonas aeruginosa. Compounds having an ethyl group showed the best activity with MIC value of 31.25 µg/mL againstStaphylococcus aureusandStreptococcus fasciens.

scholarly journals Synthesis, Characterization, and Antimicrobial Activity of Methyl-2-aminopyridine-4-carboxylate Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
S. Nagashree ◽  
P. Mallu ◽  
L. Mallesha ◽  
S. Bindya
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Studies ◽  
H Nmr ◽  
Chemical Structures ◽  
Elemental Analyses ◽  
Ft Ir

A series of methyl-2-aminopyridine-4-carboxylate derivatives,3a–f,were synthesized in order to determine theirin vitroantimicrobial activity. The chemical structures of the synthesized compounds were confirmed by elemental analyses, FT-IR, and1H NMR spectral studies. Among the synthesized compounds,3cand3dshowed good antimicrobial activity compared to other compounds in the series.

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