Preparation,Characterization and Study of Biological Activity for some new derivatives Mannich's bases derived from Shiff's bases

2021 ◽  
pp. 6025-6032
Author(s):  
Nadia Sadiq Majeed ◽  
Nada Ali Saleh ◽  
Radhiyah Abd AL-Baqi Aldujaili
Keyword(s):  
Staphylococcus Aureus ◽  
Biological Activity ◽  
Proteus Mirabilis ◽  
Aromatic Amines ◽  
Mannich Bases ◽  
Gram Negative ◽  
E Coli ◽  
The Third ◽  
Ft Ir ◽  
Shiff Bases

This paper involves synthesis new Mannich bases derived from Shiff' bases which prepared from isatin by the reaction of isatin with different aromatic amines to prepare Shiff bases derivatives (M, G, B, R, X, S), then Shiff's bases derivatives reacted with formaldehyde and piperazine to produce Mannich bases derivatives (M1, G1, B1, R1, X1, S1). The third step included the assay of biological activity of all compounds against four types of pathogens bacteria (Staphylococcus aureus, Granutice tella adiacens) gram positive and (E. coli, Proteus mirabilis) gram negative the results exhibited excellent biological activity for all derivatives compared to antibiotics (Ampicillin and Ciprofloxacin) these structures were identified by FT-IR,1HNMRand 13CNMR.

Synthesis of Chalcones and Nucleosides Incorporating [1, 3, 4]Oxadiazolenone Core and Evaluation of their Antifungal and Antibacterial Activities

2020 ◽  
Vol 15 (6) ◽  
pp. 665-679
Author(s):  
Alok K. Srivastava ◽  
Lokesh K. Pandey
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Bacillus Subtilis ◽  
Antifungal Activity ◽  
Aspergillus Niger ◽  
Gram Negative ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Good Antibacterial Activity

Background: [1, 3, 4]oxadiazolenone core containing chalcones and nucleosides were synthesized by Claisen-Schmidt condensation of a variety of benzaldehyde derivatives, obtained from oxidation of substituted 5-(3/6 substituted-4-Methylphenyl)-1, 3, 4-oxadiazole-2(3H)-one and various substituted acetophenone. The resultant chalcones were coupled with penta-O-acetylglucopyranose followed by deacetylation to get [1, 3, 4] oxadiazolenone core containing chalcones and nucleosides. Various analytical techniques viz IR, NMR, LC-MS and elemental analysis were used to confirm the structure of the synthesised compounds.The compounds were targeted against Bacillus subtilis, Staphylococcus aureus and Escherichia coli for antibacterial activity and Aspergillus flavus, Aspergillus niger and Fusarium oxysporum for antifungal activity. Methods: A mixture of Acid hydrazides (3.0 mmol) and N, Nʹ- carbonyl diimidazole (3.3 mmol) in 15 mL of dioxane was refluxed to afford substituted [1, 3, 4]-oxadiazole-2(3H)-one. The resulted [1, 3, 4]- oxadiazole-2(3H)-one (1.42 mmol) was oxidized with Chromyl chloride (1.5 mL) in 20 mL of carbon tetra chloride and condensed with acetophenones (1.42 mmol) to get chalcones 4. The equimolar ratio of obtained chalcones 4 and β -D-1,2,3,4,6- penta-O-acetylglucopyranose in presence of iodine was refluxed to get nucleosides 5. The [1, 3, 4] oxadiazolenone core containing chalcones 4 and nucleosides 5 were tested to determined minimum inhibitory concentration (MIC) value with the experimental procedure of Benson using disc-diffusion method. All compounds were tested at concentration of 5 mg/mL, 2.5 mg/mL, 1.25 mg/mL, 0.62 mg/mL, 0.31 mg/mL and 0.15 mg/mL for antifungal activity against three strains of pathogenic fungi Aspergillus flavus (A. flavus), Aspergillus niger (A. niger) and Fusarium oxysporum (F. oxysporum) and for antibacterial activity against Gram-negative bacterium: Escherichia coli (E. coli), and two Gram-positive bacteria: Staphylococcus aureus (S. aureus) and Bacillus subtilis(B. subtilis). Result: The chalcones 4 and nucleosides 5 were screened for antibacterial activity against E. coli, S. aureus and B. subtilis whereas antifungal activity against A. flavus, A. niger and F. oxysporum. Compounds 4a-t showed good antibacterial activity whereas compounds 5a-t containing glucose moiety showed better activity against fungi. The glucose moiety of compounds 5 helps to enter into the cell wall of fungi and control the cell growth. Conclusion: Chalcones 4 and nucleosides 5 incorporating [1, 3, 4] oxadiazolenone core were synthesized and characterized by various spectral techniques and elemental analysis. These compounds were evaluated for their antifungal activity against three fungi; viz. A. flavus, A. niger and F. oxysporum. In addition to this, synthesized compounds were evaluated for their antibacterial activity against gram negative bacteria E. Coli and gram positive bacteria S. aureus, B. subtilis. Compounds 4a-t showed good antibacterial activity whereas 5a-t showed better activity against fungi.

scholarly journals An unusual case of chest pain

2020 ◽  
Vol 7 (8) ◽  
pp. 1290
Author(s):  
Saswat Subhankar ◽  
K. Madhuri ◽  
Vivek D. Alone
Keyword(s):  
Staphylococcus Aureus ◽  
Developing Countries ◽  
Chest Pain ◽  
Unusual Case ◽  
Gram Negative Bacteria ◽  
Pleural Effusions ◽  
Gram Negative ◽  
Competent Patient ◽  
E Coli ◽  
Gram Positive Bacteria

Osteomyelitis is an infection of the bones caused by pyogenic organisms. The ribs are an extremely uncommon site for osteomyelitis, occurring in less than 1% cases. The main causative organisms are Gram-positive bacteria, such as Staphylococcus aureus and Hemophilus influenzae. Gram-negative bacteria like E. coli have been rarely reported. Authors hereby present a case of an immune-competent patient who presented with an osteomyelitis of the ribs caused by the latter. In developing countries, tuberculosis is considered as the primary cause of osteomyelitis and pleural effusions. However, other organisms should also be considered in patients who present with fulminant infections.

scholarly journals PREPARASI DAN MODIFIKASI KIMIA STRUKTUR KITOOLIGOSAKARIDA-2,5-ANHIDRO-D-MANNOFURANOSA (KOSAMF) DARI KITOSAN SERTA UJI ANTIBAKTERI TERHADAP Staphylococcus aureus DAN Escherichia coli

2016 ◽  
Vol 9 (2) ◽  
pp. 15
Author(s):  
Emil Salim ◽  
Hasnirwan ◽  
Sanusi Ibrahim ◽  
Afrizal
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
One Pot ◽  
E Coli ◽  
Ft Ir

Kitooligosakarida-2,5-anhidro-D-mannofuranosa (KOSamf) dipersiapkan dengan derajat polimerisasi tertentu melalui reaksi nitrous deaminasi dari kitosan parsial N-deasetilasi. KOSamf kemudian diubah menjadi turunan KOSamf dengan mengkopling gugus aldehid yang terdapat pada unit 2,5-anhidro-D-mannofuranosa (amf). KOSamf dengan 3,5-dikloroanilin dan NaBH3CN dalam pelarut buffer ammonium asetat direaksikan melalui metoda one-pot aminasi reduktif untuk menghasilkan turunan KOSamf yang berpotensi sebagai senyawa antibakteri dan antijamur. Struktur kimia dari turunan KOSamf yang telah disintesis dikarakterisasi dengan Spektroskopi FT-IR dan NMR. Senyawa turunan KOSamf memiliki aktivitas sebagai antibakteri terhadap bakteri Staphylococcus aureus dengan zona inhibisi 12,5 mm dan bakteri E. coli dengan zona inhibisi 10,5 mm.

scholarly journals Synthesis of Some New Nucleoside Analogues Containing Seven Membered Ring and Studying Their Biological Activity

2016 ◽  
Vol 13 (3) ◽  
pp. 531-546
Author(s):  
Baghdad Science Journal
Keyword(s):  
Antibacterial Activity ◽  
Membered Ring ◽  
Nucleoside Analogues ◽  
Second Step ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
The Third ◽  
Ft Ir ◽  
Fourth Step ◽  
Propiolic Acid

In this work, a series of new Nucleoside analogues (D-galactopyranose linked to oxepanebenzimidazole moiety) was synthesized via multisteps synthesis. The first step involved preparation of two benzimidazoles 2-styrylbenzimidazole and 2-(phenyl ethynyl) benzimidazole via reaction of phenylenediamine with cinnamic acid or ?-phenyl propiolic acid. Electrophilic addition of the prepared benzimidazoles by three anhydrides in the second step afforded (4-6) and (14-16) which in turn were treated with 1,2,3,4-di-O-isopropylidene galactopyranose in the third step to afford a series of the desirable protected nucleoside analogues (7-9) ,(17-19)which after hydrolysis in methanolic sodium methoxidein the fourth step afforded the free nucleoside analogues (10-12) and (20-22) .The synthesized compounds were identified by FT-IR and some of them by 1H-NMR and13C-NMR. The synthesized oxepane nucleoside analogues were screened for their antibacterial activity against three types of bacteria including Staphylococcusaureus ,Bacillus(gram positive) andE.coli (gram negative) bacteria repectively.

Morpholine- and Thiomorpholine-Based Amidodithiophosphonato Nickel Complexes: Synthesis, Characterization, P–N Cleavage, Antibacterial Activity and Silica Nano-Dispersion

2021 ◽  
Vol 21 (5) ◽  
pp. 2879-2891
Author(s):  
Enrico Podda ◽  
M. Carla Aragoni ◽  
Massimiliano Arca ◽  
Giulia Atzeni ◽  
Simon J. Coles ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Nickel Complex ◽  
Nickel Complexes ◽  
Silica Matrix ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
Ft Ir ◽  
Hydrolysis Of

The reactivity of thiomorpholinium P-(4-methoxyphenyl)-N-thiomorpholin-amidodithiophosphonate (S-MorH+2)(S-Mor-adtp−) and morpholinium P-(4-methoxyphenyl)-N-morpholin-amidodithiophosphonate (O-MorH+2)(O-Mor-adtp−) towards nickel (II) dichloride hexahydrated is presented and the hydrolysis of the relevant metal complexes investigated. The hydrolytic products (S-MorH+2)2 [Ni(dtp)2]2− and (O-MorH+2)2[Ni(dtp)2]2− were characterized by means of FT-IR, 1H, and 31P NMR and XRD and the experimented P–N cleavage investigated and elucidated by means of DFT calculations. The antimicrobial activity of the neutral nickel complex [Ni(S-Mor-adtp)2] was tested against a set of Gram-positive and Gram-negative bacteria alongside with its nanodispersion in a silica matrix. The complex [Ni(S-Mor-adtp)2] did not show antibacterial activity, whilst the nano-dispersed sample [Ni(S-Mor-adtp)2]_SiO2 demonstrated inhibition to growth of Staphylococcus aureus. The nanocomposites were fully characterized by means of XRPD, TGA, SEM and dinitrogen sorption techniques.

scholarly journals Graphene oxide-based electrochemical activation of ethionamide towards enhanced biological activity

RSC Advances ◽  
2019 ◽  
Vol 9 (61) ◽  
pp. 35463-35472 ◽  
Author(s):  
Balaji B. Mulik ◽  
Sambhaji T. Dhumal ◽  
Vijay S. Sapner ◽  
Naziya N. M. A. Rehman ◽  
Prashant P. Dixit ◽  
...  
Keyword(s):  
Biological Activity ◽  
Graphene Oxide ◽  
Electrochemical Activation ◽  
Ftir Analysis ◽  
Gram Negative ◽  
E Coli ◽  
Oxidative Activation

Electrochemical oxidative activation of ethionamide (ETO) on GO (∼500 nm) confirmed by HRMS and FTIR analysis. The ETO-O (oxidized form) showed enhancement in activity over ETO against Gram negative pathogens (E. aerogenes, S. abony, S. boydii, E. coli).

scholarly journals Green synthesis of Ag, Zn and Cu nanoparticles from aqueous extract of Spondias mombin leaves and evaluation of their antibacterial activity

2020 ◽  
Vol 21 (2) ◽  
pp. 106-113
Author(s):  
D.K. Adeyemi ◽  
A.O. Adeluola ◽  
M.J. Akinbile ◽  
O.O. Johnson ◽  
G.A. Ayoola
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Green Synthesis ◽  
Antimicrobial Activities ◽  
Cu Nanoparticles ◽  
E Coli ◽  
Spondias Mombin ◽  
Ft Ir ◽  
Uv Visible

Background: Nanotechnology offers an advantage as a green route for synthesis of metal nanoparticles (NPs) with plant extracts as capping agent. Spondias mombin is a fruit-bearing tree and its leaf extracts have been reported to possess anxiolytic, hypoglycaemic, antiepileptic, antipsychotic, sedative, antioxidant, and antimicrobial properties. The objective of the study is to determine the antibacterial potential of a simple non-toxic product of green synthesis of metallic (Ag, Zn and Cu) nanoparticles using the leaf of Spondias mombin aqueous extracts (SMAE) as a reducing and capping agents of the metal ions.Methodology: Nanoparticles were characterized by UV visible spectrophotometeric analysis, Fourier Transform Infra-Red (FT-IR) spectrophotometer and scanning electron microscope (SEM). Antimicrobial activities of synthesized NPs against Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa were determined by agar well diffusion technique.Results: The synthesized NPs varied in colour from dark brown to green and appears dominantly spherical, occasionally rod or triangular shaped with size ranging from 65-90 nm. UV spectroscopy absorption spectra of Ag, Zn and Cu NPs had absorbance peak at 267, 262 and 765 nm respectively. FT-IR spectrometry of Zn NP, Cu NP, and SMAE gave wave number ranging from 895.71-3320.67, 747.02-3225.45 and 658.25-3674.49 respectively. FT-IR analysis showed that SMAE acted as reducing and stabilizing agent while the NPs exhibited lower energy absorption band when compared to the plant extract. The NPs demonstrated higher antimicrobial activities against S. aureus than Ps. aeruginosa and E. coli. The antimicrobial activity was higher with copper NP than Ag and Zn NPs, and also higher than SMAE.Conclusion: The result from this study presents an indication for an alternative means for development of novel antimicrobial agents for clinical and biotechnological applications.Keywords: synthesis, nanoparticles, FT-IR, UV-visible spectrophotometry, antibacterial activitiesFrench Title: Synthèse verte de nanoparticules d'Ag, de Zn et de Cu à partir d'extrait aqueux de feuilles de Spondias mombin et évaluation de leur activité antibactérienneContexte: La nanotechnologie offre un avantage en tant que voie verte pour la synthèse de nanoparticules métalliques (NP) avec des extraits de plantes comme agent de coiffage. Spondias mombin est un arbre fruitier et ses extraits de feuilles possèdent des propriétés anxiolytiques,  hypoglycémiques, antiépileptiques, antipsychotiques, sédatives,  antioxydantes et antimicrobiennes. L’objectif de l’étude est de déterminer le potentiel antibactérien d’un simple produit non toxique de synthèse verte de nanoparticules métalliques (Ag, Zn et Cu) à l’aide de la feuille d’extraits aqueux de Spondias mombin (SMAE) en tant qu’agent réducteur et coiffant de la ions métalliques.Méthodologie: Les nanoparticules ont été caractérisées par analyse  spectrophotométrique UV visible, spectrophotomètre à transformée de Fourier infrarouge (FT-IR) et microscope électronique à balayage (MEB). Lesactivités antimicrobiennes de NP synthétisées contre Escherichia coli, Staphylococcus aureus et Pseudomonas aeruginosa ont été déterminées par une technique de diffusion sur puits d’agar.Résultats: Les NP synthétisés ont une couleur allant du brun foncé au vert et apparaissent principalement sphériques, parfois en bâtonnets ou en triangles, avec des tailles allant de 65 à 90 nm. Les spectres  d'absorption par spectroscopie UV des NP Ag, Zn et Cu présentaient des pics  d'absorbance à 267, 262 et 765 nm respectivement. La spectrométrie FT-IR de Zn NP, Cu NP et SMAE a donné un nombre d'onde allant de 895,71 à 3320,67, 747,02 à 3225,45 et 658,25 à 3674,49 respectivement. L'analyse FT-IR a montré que le SMAE agissait en tant qu'agent réducteur et  stabilisant, alors que les NP présentaient une bande d'absorption d'énergie inférieure à celle de l'extrait de plante. Les NP ont démontré des activités antimicrobiennes plus élevées contre S. aureus que Ps. aeruginosa et E. coli. L'activité antimicrobienne était plus élevée avec les NP en cuivre que dans les NP Ag et Zn, et également supérieure à celle du SMAE.Conclusion: le résultat de cette étude présente une indication d'un autre moyen de développement de nouveaux agents antimicrobiens pour des applications cliniques et biotechnologiques.Mots-clés: synthèse, nanoparticules, FT-IR, spectrophotométrie UV-visible, activités antibactériennes 

scholarly journals An Efficient Disinfectant, Composite Material {SLS@[Zn3(CitH)2]} as Ingredient for Development of Sterilized and Non Infectious Contact Lens

Antibiotics ◽  
2019 ◽  
Vol 8 (4) ◽  
pp. 213 ◽  
Author(s):  
V.A. Karetsi ◽  
C.N. Banti ◽  
N. Kourkoumelis ◽  
C. Papachristodoulou ◽  
C.D. Stalikas ◽  
...  
Keyword(s):  
Contact Lenses ◽  
Fluorescence Analysis ◽  
Gram Positive ◽  
Gram Negative ◽  
X Ray ◽  
E Coli ◽  
X Ray Crystallography ◽  
Ft Ir ◽  
And Staphylococcus Aureus ◽  
Ft Raman

The [Zn3(CitH)2] (1) (CitH4= citric acid), was dispersed in sodium lauryl sulphate (SLS) to form the micelle of SLS@[Zn3(CitH)2] (2). This material 2 was incorporated in hydrogel made by hydroxyethyl-methacrylate (HEMA), an ingredient of contact lenses, toward the formation of pHEMA@(SLS@[Zn3(CitH)2]) (3). Samples of 1 and 2 were characterized by UV-Vis, 1H-NMR, FT-IR, FT-Raman, single crystal X-ray crystallography, X-ray fluorescence analysis, atomic absorption and TG/DTA/DSC. The antibacterial activity of 1–3 as well as of SLS against Gram-positive (Staphylococcus epidermidis (St. epidermidis) and Staphylococcus aureus (St. aureus)) and Gram-negative (Pseudomonas aeruginosa (PAO1), and Escherichia coli (E. coli)) bacteria was evaluated by the means of minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC) and inhibitory zone (IZ). 2 showed 10 to 20-fold higher activity than 1 against the bacteria tested. Moreover the 3 decreases the abundance of Gram-positive microbes up to 30% (St. aureus) and up to 20% (PAO1) the Gram-negative ones. The noteworthy antimicrobial activity of the obtained composite 3 suggests an effective antimicrobial additive for infection-free contact lenses.

Synthesis and in vitro Biological Activity of New 4,6-Disubstituted 3(2H)-Pyridazinone-acetohydrazide Derivatives

2012 ◽  
Vol 67 (5-6) ◽  
pp. 257-265
Author(s):  
Murat Sukuroglu ◽  
Tijen Onkol ◽  
Fatma Kaynak Onurdağ ◽  
Gulsen Akalın ◽  
M. Fethi Şahin
Keyword(s):  
Biological Activity ◽  
Antimicrobial Activities ◽  
Cytotoxic Activities ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
E Coli ◽  
Preliminary Results ◽  
H Nmr ◽  
Pyridazinone Derivatives

New 3(2H)-pyridazinone derivatives containing a N’-benzyliden-acetohydrazide moiety at position 2 were synthesized. The structures of these newly synthesized compounds were confi rmed by IR, 1H NMR, and MS data. These compounds were tested for their antibacterial, antifungal, antimycobacterial, and cytotoxic activities. The compounds 2-[4-(4-chlorophenyl)- 6-(morpholin-4-yl)-3-oxo-(2H)-pyridazin-2-yl]-N’-(4-tert-butylbenzyliden)acetohydrazide and 2-[4-(4-chlorophenyl)-6-(morpholin-4-yl)-3-oxo-(2H)-pyridazin-2-yl]-N’-(4-chlorobenzyliden) acetohydrazide exhibited activity against both Gram-positive and Gram-negative bacteria. Most of the compounds were active against E. coli ATCC 35218. The preliminary results of this study revealed that some target compounds exhibited promising antimicrobial activities

scholarly journals Burdock (Arctium lappa) Leaf Extracts Increase the In Vitro Antimicrobial Efficacy of Common Antibiotics on Gram-positive and Gram-negative Bacteria

2017 ◽  
Vol 15 (1) ◽  
pp. 92-102 ◽  
Author(s):  
Lucia Pirvu ◽  
Isabela Nicorescu ◽  
Cristina Hlevca ◽  
Bujor Albu ◽  
Valentin Nicorescu
Keyword(s):  
Staphylococcus Aureus ◽  
Ethanol Extract ◽  
Leaf Extracts ◽  
Gram Positive ◽  
Polyphenol Compounds ◽  
Arctium Lappa ◽  
Gram Negative ◽  
E Coli ◽  
Polar Extracts

AbstractThis work aimed to study the potential effects of four Arctii folium extracts, 5 mg gallic [GAE] acid equivalents per 1 mL sample, on six antibiotics (Ampicillin/AM, Tetracycline/TE, Ciprofloxacin/CIP, Sulfamethoxazole-Trimethoprim/SXT, Chloramphenicol/C and Gentamicin/CN) tested on four Gram-positive (Staphylococcus aureus ATCC 6538, Staphylococcus aureus ATCC 25923, Enterococcus faecalis ATCC 29212, and Staphylococcus epidermidis ATCC 12228) and five Gram-negative (Proteus mirabilis ATCC 29245, Escherichia coli ATCC 35218, E. coli ATCC 11229, E. coli ATCC 8739, and Bacillus cereus ATCC 11778) bacteria. Arctii folium extracts were the whole ethanol extract/W and subsequent ethyl acetate/EA, aqueous/AQ, and chloroform/CHL fractions. Chemical qualitative analysis (HPTLC method) emphasized five main polyphenol compounds in Arctii folium polar extracts: chlorogenic acid (Rf≈0.52/0.55) and its isomer, 1,5-di-O-caffeoylquinic acid (Rf≈0.90/0.92), plus cynarin (Rf≈0.77), hyperoside (Rf≈0.68/0.64) and isoquercitrin (Rf≈0.69/0.71). Microbiological screening indicated Arctii folium polar extracts (AQ and W) efficacy on S. epidermidis ATCC 12228; the MIC values were in the range of common antibiotics, being 32 and 128 μg GAE per mL sample respectively. The unpredictable effects (stimulatory or inhibitory) of Arctii folium extracts in combination with typical antibiotics as well as a potential use of the whole ethanol extract/W for restoring the antimicrobial potency of susceptible antibiotics have also been evidenced.

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