Pyrroloimidazolediones Derived from Aminomalonates and Benzaldehydes

Synlett ◽  
2021 ◽  
Author(s):  
Mark G. Moloney ◽  
Lewis O’Shaughnessy ◽  
Charles Hutchinson ◽  
Adam Waldron ◽  
Kirsten E. Christensen
Keyword(s):  
Antibacterial Activity ◽  
Ring Closure ◽  
Metal Chelating ◽  
Bicyclic Lactams ◽  
Substituted Benzaldehydes

AbstractBicyclic lactams can be prepared from diethyl aminomalonate and substituted benzaldehydes by formation of a dimerised imidazolidine cycloadduct followed by a Dieckmann ring closure. The resulting N,N-heterocycles are metal-chelating but show no antibacterial activity.

Synthesis of Chiral Bicyclic Lactams Using Ring Closure Metathesis: Synthesis of (-)-Coniceine and (S)-Pyrrolam A

Synlett ◽  
1997 ◽  
Vol 1997 (10) ◽  
pp. 1179-1180 ◽  
Author(s):  
Mitsuhiro Arisawa ◽  
Emiko Takezawa ◽  
Atsushi Nishida ◽  
Miwako Mori ◽  
Masako Nakagawa
Keyword(s):  
Ring Closure ◽  
Bicyclic Lactams

ChemInform Abstract: Synthesis of Chiral Bicyclic Lactams Using Ring Closure Metathesis: Synthesis of (-)-Coniceine and (S)-Pyrrolam A.

ChemInform ◽  
2010 ◽  
Vol 29 (5) ◽  
pp. no-no
Author(s):  
M. ARISAWA ◽  
E. TAKEZAWA ◽  
A. NISHIDA ◽  
M. MORI ◽  
M. NAKAGAWA
Keyword(s):  
Ring Closure ◽  
Bicyclic Lactams

Nuclear analogs of β-lactam antibiotics. II. Synthesis of O-2-isocephems

1977 ◽  
Vol 55 (3) ◽  
pp. 484-507 ◽  
Author(s):  
Terrence W. Doyle ◽  
Bernard Belleau ◽  
Bing-Yu Luh ◽  
Terry Thomas Conway ◽  
Marcel Menard ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Total Synthesis ◽  
Spectral Characteristics ◽  
Ring Closure ◽  
Phenoxyacetic Acid ◽  
New Class ◽  
High Antibacterial Activity ◽  
Hydrolysis Of

The preparation by total synthesis of a new class of β-lactam antibiotics is reported. Conversion of alcohol 1b to its mesylate 9b followed by hydrolysis of the acetal to the enol 1b and base-catalyzed ring closure gave benzyl 7- β-azido-Δ3-O-2-isocephem-4-carboxylate 8b. Similarly prepared were the 3 -methyl, 3 -benzyl, and 3 -phenethyl analogs (32b–d). Reduction of the azides followed by coupling of the resultant amines with phenoxyacetic acid and removal of the benzyl groups by hydrogenolysis gave the acids 35a–e which exhibited high antibacterial activity. The structural assignments to the O-2-isocephems which were made on the basis of their spectral characteristics (ir, uv, and nmr) are discussed.

scholarly journals Synthesis, Characterization and Antibacterial Activity Study of Cobalt(II), Nickel(II), Copper(II), Palladium(II), Cadmium(II) and Platinum(IV) Complexes with 4-Amino-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazole-3-thione

2021 ◽  
Vol 21 (6) ◽  
pp. 1514
Author(s):  
Waleed Abbas Jawad ◽  
Asim Alaa Abd Al-Hussein Balakit ◽  
Mahmoud Najim Abid Al-Jibouri
Keyword(s):  
Antibacterial Activity ◽  
Metal Complexes ◽  
Thermal Analyses ◽  
Free Ligand ◽  
Molar Conductance ◽  
Bidentate Ligand ◽  
Ring Closure ◽  
Tetrahedral Geometry ◽  
Visible Spectra ◽  
Elemental Analyses

New transition metal complexes of cobalt(II), nickel(II), copper(II), palladium(II), cadmium(II), and platinum(IV) with bidentate ligand 4-amino-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazole-3-thiol were synthesized and characterized by microelemental analyses (CHNS), Fourier-transform infrared (FT-IR), UV-Visible spectra, molar conductance, magnetic susceptibility and thermal analyses (TG-DSC). The ligand was synthesized by ring closure of potassium-2-(3,4,5-trimethoxybenzoyl) hydrazine carbodithioate with an excess amount of hydrazine, and then was acidified using hydrochloric acid. The ligand was used as Lewis bases to prepare metal complexes through the reaction of ratio (1:2) metal:ligand. The ligand was characterized by 1H-NMR and 13C-NMR and the previously described methods to identify the complexes. The results obtained from spectra and elemental analyses indicated the tetrahedral geometry around Cd(II) ion, square-planar for Cu(II) and Pd(II), and octahedral geometry around Co(II), Ni(II), and Pt(IV). All the metal complexes showed significant antibacterial activity in comparison with the free ligand. The antibacterial test of the platinum(IV) complex showed higher activity than other metal complexes against bacteria Staphylococcus aureus (G-positive) and Escherichia coli (G-negative).

scholarly journals Synthetic studies of Alkoxy isoindole-1,3-diones tetra-azabenzo[f]azulenes and their Antibacterial activity

2006 ◽  
Vol 3 (1) ◽  
pp. 28-34
Author(s):  
M. Ahmed ◽  
R. Sharma ◽  
D. P. Nagda ◽  
V. K. Salvi ◽  
G. L. Talesara
Keyword(s):  
Antibacterial Activity ◽  
Spectral Data ◽  
Elemental Analysis ◽  
Sodium Acetate ◽  
Antibacterial Properties ◽  
Anhydrous Sodium Acetate ◽  
Bacterial Strains ◽  
Substituted Benzaldehydes ◽  
Synthetic Studies

3-Methylpyrazol-5-one3reacts with substituted benzaldehydes4a-din the presence of anhydrous sodium acetate to produce the corresponding 4-arylidene-5-methyl-2,4-dihydro-pyrazol-3-ones5a-dand the condensation of5a-dwith 2-bromoalkoxy-1H-isoindole-1, 3-(2H)-diones2a-cfurnished corresponding 2-[2-(4-arylidene-3-methyl-5-oxo-4,5-dihydro-pyrazol-1-yl)alkoxy]-isoindole-1,3-diones6a-l, which on cyclisation with o-phenylendiamine give titled compounds7a-l. All the synthesized compounds have been characterized by elemental analysis and spectral data and screened for their antibacterial properties against various bacterial strains in order to obtain chemotherapeutic properties.

Essential Oil and Ethanol Extract of Oregano (Origanum vulgare L.) from Armenian Flora as a Natural Source of Terpenes, Flavonoids and other Phytochemicals with Antiradical, Antioxidant, Metal Chelating, Tyrosinase Inhibitory and Antibacterial Activity

2019 ◽  
Vol 25 (16) ◽  
pp. 1809-1816 ◽  
Author(s):  
Armenuhi Moghrovyan ◽  
Naira Sahakyan ◽  
Anush Babayan ◽  
Naira Chichoyan ◽  
Margarit Petrosyan ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Essential Oil ◽  
Antibacterial Properties ◽  
Ethanol Extract ◽  
Natural Source ◽  
Origanum Vulgare ◽  
Oregano Essential Oil ◽  
E Coli ◽  
Metal Chelating

Background: Origanum vulgare is used in Armenian cuisine as well as in folk medicine. The aim of this investigation was to determine the peculiarities of the chemical composition of Armenian flora’s oregano essential oil (EO) and ethanol extract (EE) and to characterize mainly antioxidant and antibacterial properties in vitro. Methods: EO of plant aerial parts was extracted by the hydro-distillation method, and the composition was analyzed by gas-chromatography (GC). EE was prepared using ethanol as a solvent. Antioxidant, antibacterial and other biological activity of EO and EE was determined using appropriate methods. Results: The terpenes were found to be the greatest part of oregano EO (β-caryophyllene epoxide - 13.3 %; β- caryophyllene -8.2 %; ο-cymene - 5.2 %). The flavonoid content of EE was 3.9±0.7 mg g-1 catechin equivalents. Antiradical activities of EO and EE expressed with half-maximum inhibitory concentrations were 1057 µg mL-1 and 19.97 µg mL-1. The antioxidant index in the case of using extract (1000 µg mL-1) was 77.3±1.5 %. The metal chelating activity of EE was 74.5±0.2 %. The tyrosinase inhibitory activities of EO, EE and arbutin were 26.5±0.3 %, 6.5±0.2 % and 50±0.1 %, respectively. Both EO and EE of oregano were able to suppress the growth of testmicroorganisms including clinical pathogen isolates, but have moderate antimicrobial activity. EO antibacterial activity against ampicillin-resistant Escherichia coli was similar to the activity against non-resistant strain. EE was not active against ampicillin-resistant E. coli in contrast to non-resistant one. Conclusion: The results indicate high antioxidant and moderate antibacterial as well as high antiradical, metal chelating, tyrosinase inhibitory activity of oregano EO and EE, which can be used as a natural source of terpenes, flavonoids and other phytochemicals in medicine, pharmaceutics, cosmetics and food industry. EO has antibacterial activity also against ampicillin-resistant E. coli.

Preparation and antibacterial activity of Schiff bases from O-carboxymethyl chitosan and para-substituted benzaldehydes

2011 ◽  
Vol 68 (5) ◽  
pp. 1215-1226 ◽  
Author(s):  
Xueqiong Yin ◽  
Junhua Chen ◽  
Wen Yuan ◽  
Qiang Lin ◽  
Li Ji ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Schiff Bases ◽  
Carboxymethyl Chitosan ◽  
Substituted Benzaldehydes

scholarly journals In vitro antioxidant and antimicrobial activity of carotenoid pigment extracted from Sporobolomyces sp. isolated from natural source

2014 ◽  
Vol 6 (2) ◽  
pp. 649-653 ◽  
Author(s):  
M. R. A. Manimala ◽  
R. Murugesan
Keyword(s):  
Antibacterial Activity ◽  
Antioxidant Activities ◽  
Steady Increase ◽  
Carotenoid Pigment ◽  
E Coli ◽  
Chelating Activity ◽  
Metal Chelating ◽  
Potential Source ◽  
Antioxidant And Antimicrobial Activity

The aim of the present study was to isolate and study about the antioxidant and antibacterial activity of carotenoid pigment. Sporobolomyces sp. isolated from the phyllosphere surface of rice plant has found to produce carotenoid pigment. The present investigation was carried out for antioxidant assays viz., DPPH, iron reducing and metal chelating activity. A steady increase in the antioxidant activities was observed in the carotenoid pigment with raising the pigment concentration. In the present study, the maximum antioxidation characteristics of carotenoid by DPPH, iron reducing and metal chelating assays (75.04 %, 1.88 % and 59.32 %) were achieved by pigmentation of Sporobolomyces sp. at the concentration of 100 μg ml-1. The antibacterial activity was studied on several organisms like Enterococcus sp., Staphylococcus aureus, Streptococcus faecalis, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa. Among the six pathogens, the pigment was found to be more effective against E. coli (2.9 cm) and S. aureus (2.6 cm). This study revealed that yeast carotenoid pigment was a potential source for its use in food and pharmaceutical applications.

Antibacterial activity of herbal preparation to treat sore throats

Planta Medica ◽  
2008 ◽  
Vol 74 (09) ◽  
Author(s):  
J Reichling ◽  
U Suschke ◽  
A Suter
Keyword(s):  
Antibacterial Activity ◽  
Herbal Preparation
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