scholarly journals Synthesis of Sulfonated Dihydrofuropyrazoles Derivatives as Antimicrobial Active Agents

2019 ◽  
Vol 31 (4) ◽  
pp. 773-779 ◽  
Author(s):  
Venkata Swamy Tangeti ◽  
K.V.V.V. Satyanarayana

A series of sulfonyl dihydrofuropyrazole derivatives was prepared from one pot multi component condensation of sulfonated β-keto ester, aromatic aldehyde, hydrazine, pyridinium ylide in presence of piperidine catalyst under ethanol solvent conditions and subsequent oxidation of SPh group with MCPBA. All the synthesized compounds were characterized by analytical and spectral techniques and screened in vitro for antimicrobial activity. The activity data revealed that most of the compounds exhibited good to significant activities. Compounds 6b, 6i, 6j, 6k, 6m, 6n exhibited good and broad spectrum activity towards all the tested bacterial strains.

2011 ◽  
Vol 396-398 ◽  
pp. 241-245
Author(s):  
Yu Ting Liu ◽  
Ming Tao Zhao ◽  
Da Wei Yin ◽  
Bo Ning Hui

A series of novel Schiff base containing diacetylferrocene and 5-alkyl-2-amino-1,3,4 -thiodizoles were reported in this paper. Diacetylferrocene(Ⅱ) was synthesised with ferrocene(Ⅰ) and acetyl chloride with AlCl3 as catalyst in CH2Cl2. In the presence of diacetylferrocene and 5-alkyl-2-amino-1,3,4-thiodizole reacted under solvent and catalyst condition to furnish Schiff base containing diacetylferrocene and 5-alkyl-2-amino-1,3,4-thiadiazoles(Ⅲ). Chemical structures have been confirmed by elemental annalysis and the spectral techniques of FTIR,1H NMR. Antimicrobial activity (in vitro) was evaluated against the two pathogenic bacterial strains. The compounds have shown better activity.


Author(s):  
Usman Abubakar Adamu ◽  
Buhari Magaji ◽  
Muhammad Nazifi Ibrahim ◽  
Mukhtar Muhammad Sani

Schiff base was prepared by the condensation of 3-aminophenol and benzaldehyde in a 1:1 ratio and its complexes of Mn(II), Co(II) and Cu(II) were synthesized in a 1:2 ratio (Metal: Ligand) and the Schiff base and the complexes were characterized by using the different techniques. The infrared spectral data revealed that the Schiff base behaved as a bidentate ligand and the molar conductivity value indicated that the complexes were non-electrolytes. Furthermore, the in vitro antibacterial activity of the Schiff base and its complexes was evaluated against one gram-negative and one gram-positive bacteria to indicate that Mn (II) complex demonstrated a good broad-spectrum activity against all the tested bacterial strains.


Coatings ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 473
Author(s):  
Dilyana Gospodonova ◽  
Iliana Ivanova ◽  
Todorka Vladkova

The aim of this study was to prepare TiO2/Ag/Cu magnetron co-sputtered coatings with controlled characteristics and to correlate them with the antimicrobial activity of the coated glass samples. The elemental composition and distribution, surface morphology, wettability, surface energy and its component were estimated as the surface characteristics influencing the bioadhesion. Well expressed, specific, Ag/Cu concentration-dependent antimicrobial activity in vitro was demonstrated toward Gram-negative and Gram-positive standard test bacterial strains both by diffusion 21 assay and by Most Probable Number of surviving cells. Direct contact and eluted silver/coper nanoparticles killing were experimentally demonstrated as a mode of the antimicrobial action of the studied TiO2/Ag/Cu thin composite coatings. It is expected that they would ensure a broad spectrum bactericidal activity during the indwelling of the coated medical devices and for at least 12 h after that, with the supposition that the benefits will be over a longer time.


2017 ◽  
Vol 61 (8) ◽  
Author(s):  
David Wensel ◽  
Yongnian Sun ◽  
Zhufang Li ◽  
Sharon Zhang ◽  
Caryn Picarillo ◽  
...  

ABSTRACT A novel fibronectin-based protein (Adnectin) HIV-1 inhibitor was generated using in vitro selection. This inhibitor binds to human CD4 with a high affinity (3.9 nM) and inhibits viral entry at a step after CD4 engagement and preceding membrane fusion. The progenitor sequence of this novel inhibitor was selected from a library of trillions of Adnectin variants using mRNA display and then further optimized for improved antiviral and physical properties. The final optimized inhibitor exhibited full potency against a panel of 124 envelope (gp160) proteins spanning 11 subtypes, indicating broad-spectrum activity. Resistance profiling studies showed that this inhibitor required 30 passages (151 days) in culture to acquire sufficient resistance to result in viral titer breakthrough. Resistance mapped to the loss of multiple potential N-linked glycosylation sites in gp120, suggesting that inhibition is due to steric hindrance of CD4-binding-induced conformational changes.


2016 ◽  
Vol 11 (2) ◽  
pp. 248 ◽  
Author(s):  
Kathirvel Poonkodi ◽  
Subban Ravi

<p class="Abstract">The present study was aimed to evaluate the phytochemical screening and antimicrobial activity of the petroleum ether and methanol extracts from the mature leaves of <em>Richardia scabra</em> from India. Disc diffusion method was used to determine the zone inhibition of the tested samples for antibacterial and agar plug method was used to determine the antifungal activity, while the microtube-dilution technique was used to determine the minimum inhibitory concentration. Both extracts showed significant antibacterial and antifungal activities when tested against 10 bacterial and four fungal strains. The minimum inhibitory concentrations of the methanol extract of<em> R. scabra</em> ranged between 12.5–100 μg/mL for bacterial strains. Alkaloids, steroids, flavonoids, fatty acids, terpenoids and simple sugar were detected as phytoconstituents of extracts. To the best of our knowledge, this is the first report against antimicrobial activity of common weed species <em>R. scabra</em> found in India.</p><p> </p>


Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4958
Author(s):  
Jessa Marie V. Makabenta ◽  
Jungmi Park ◽  
Cheng-Hsuan Li ◽  
Aritra Nath Chattopadhyay ◽  
Ahmed Nabawy ◽  
...  

Biofilm infections are a global public health threat, necessitating new treatment strategies. Biofilm formation also contributes to the development and spread of multidrug-resistant (MDR) bacterial strains. Biofilm-associated chronic infections typically involve colonization by more than one bacterial species. The co-existence of multiple species of bacteria in biofilms exacerbates therapeutic challenges and can render traditional antibiotics ineffective. Polymeric nanoparticles offer alternative antimicrobial approaches to antibiotics, owing to their tunable physico-chemical properties. Here, we report the efficacy of poly(oxanorborneneimide) (PONI)-based antimicrobial polymeric nanoparticles (PNPs) against multi-species bacterial biofilms. PNPs showed good dual-species biofilm penetration profiles as confirmed by confocal laser scanning microscopy. Broad-spectrum antimicrobial activity was observed, with reduction in both bacterial viability and overall biofilm mass. Further, PNPs displayed minimal fibroblast toxicity and high antimicrobial activity in an in vitro co-culture model comprising fibroblast cells and dual-species biofilms of Escherichia coli and Pseudomonas aeruginosa. This study highlights a potential clinical application of the presented polymeric platform.


Author(s):  
Prasanna Habbu ◽  
Vijayanand Warad ◽  
Rajesh Shastri ◽  
Chetan Savant ◽  
Smita Madagundi ◽  
...  

Author(s):  
M. Binigha ◽  
R. Gayatri Devi ◽  
J. Selavaraj ◽  
A. Jothi Priya

Tecoma stans is a flowering plant belonging to the family Bignoniaceae. It is the floral emblem of the Bahamas. Abutilon indicum belongs to the family Malvaceae. It is also called Indian Mallow. Tecoma stans and Abutilon indicumhave antimicrobial activity and can be used in producing antibiotics. There is an urgent need to produce new antibiotics as there is an increase in the development of pathogen resistant drugs. The aim of this study was to compare the antimicrobial activity of ethanolic extract of Tecoma stansand Abutilonindicum leaves. E.faecalis bacteria were maintained in nutrient agar slopes. The powder of the two herbs, were subjected to extraction by Soxhlet extractor and was concentrated to dry residue by Agar well diffusion method. The nutrient broth was inoculated with bacterial strains. The culture was adjusted to 0.5McFarland turbidity standard. Lawn culture was done in Muller-Hinton agar plate and then the plates were dried. A 6 mm diameter well is bored for different concentrations. The extracts were introduced into the well and allowed to stand for 24 hrs. The antibacterial activity was determined by measuring the zone of inhibition. The present finding on the antimicrobial potential of Abutilon indicum and Tecoma stands showed that the two plants have growth inhibitory activity against oral pathogen E. faecalis. Abutilon indicum has a zone of inhibition greater than Tecoma stans. Abutilon indicum exhibited better activity compared to Tecoma stans.


2021 ◽  
Vol 9 (09) ◽  
pp. 900-909
Author(s):  
Anupama Srivastava ◽  
◽  
Shilpi Srivastava ◽  
Om. P. Pandey ◽  
Soumitra K. Sengupta ◽  
...  

Titanium(IV) complexes of type[(η5-C5H5)2TiCl(L)] have been synthesized by the reactions of bis(cyclopentadienyl)titanium(IV)dichloride with Schiff bases (LH) derived by the condensation of 5-(substituted aryl)-2-hydrazino-1,3,4-oxadiazole and indoline-2,3-dione in tetrahydrofuranin the presence oftriethylamine. All these complexes are soluble in PhNO2, DMF and DMSO.The complexes were characterized by elemental analyses, electrical conductance, magnetic susceptibility, UV-Vis, IR, 1H NMR, 13C NMR, XRD and SEM spectral techniques. Low molar conductance values indicate that they are non-electrolytes. The spectral data indicate5-coordinate geometry for the complexes.XRD pattern indicate that the complexes have monoclinic crystal system and particle sizes were found 49.36 nm (nano-size). In vitro antifungal activity of synthesized compounds was evaluated against fungi Aspergillusniger, Aspergillusflavus,ColletotrichumfalcatumandIn vitro antibacterial activity was determined by screening the compounds against gram negative (P. aeruginosa, S.typhi) and gram positive (S. aureus and B.subtilis) bacterial strains using minimum inhibition concentration method (MIC) by serial dilution technique. The titanocene(IV) complexes have higher antimicrobial effect than the parent Schiff bases.


Sign in / Sign up

Export Citation Format

Share Document