scholarly journals One-Pot Synthesis of Some Novel N-Aryl-1,4-Dihydropyridines Derivatives Bearing Nitrogen Mustard

Author(s):  
P.M. Singala ◽  
Viresh H. Shah

The synthesis of a novel dihydropyridine, bearing carbethoxy groups at C(3) and C(5), respectively, has been achieved by applying three component Hantzsch-type condensation. The products were assayed for their in vitro biological assay antibacterial activity against with two Gram-positive bacteria Staphylococcus aureus MTCC-96, Streptococcus pyogenes MTCC 443, two Gram-negative bacteria Escherichia coli MTCC 442, Pseudomonas aeruginosa MTCC 441 and three fungal strains Candida albicans MTCC 227, Aspergillus Niger MTCC 282, Aspergillus clavatus MTCC 1323 taking ampicillin, chloramphenicol, ciprofloxacin, norfloxacin, nystatin, and griseofulvin as standard drugs.

2020 ◽  
Vol 5 (1) ◽  
pp. 1-5
Author(s):  
K. Kapadiya ◽  
G. Dubal ◽  
Y. Bhola ◽  
P. Dholaria

A new series of 4-((5-(2-chlorophenyl)-1,3,4-oxadiazol-2-yl)methoxy)-N-(benzylidene derivatives)benzenamine (5a-k) have been synthesized and were screened for their in vitro antibacterial activity against Gram-positive bacteria (Pseudomonas aeruginosa, Streptococcus pyogenes), Gram-negative bacteria (Escherichia coli, Staphylococcus aureus) and antifungal activity (Candida albicans, Aspergillus niger, Aspergillus clavatus). Synthesized compounds were characterized by IR, mass (MS), 1H NMR and 13C NMR spectra. The synthesized compounds 5b, 5c, 5g and 5i showed potency in terms of antimicrobial activity against tested microorganisms.


2013 ◽  
Vol 78 (9) ◽  
pp. 1323-1333 ◽  
Author(s):  
Garima Matela ◽  
Robina Aman ◽  
Chetan Sharma ◽  
Smita Chaudhary

A new series of diisopropyloxytin- and triorganotin(IV) complexes of H2hbgl (1) of the general formula Sn(OPri)2(hbgl) (2), Sn(OPri)2(Hhbgl)2 (3), Ph3Sn(Hhbgl) (4), Bu3Sn(Hhbgl) (5) and Me3Sn(Hhbgl) (6), [where H2hbgl= a ligand of thymol derivative namely, N-(2-hydroxy-3-isopropyl-6-methyl benzyl)Glycine] were synthesized by reacting tin- and triorganotin(IV) chloride with the ligand, with the aid of sodium iso-propoxide in appropriate stiochiometric ratios (1:1 and 1:2). These complexes were characterized by elemental analysis, IR, 1H nuclear magnetic resonance. The spectral data suggest that the carboxylate group, in complexes 2-5, was bonded in a bidentate manner, while a unidentate bonding was observed in complex 6. All five complexes were tested in vitro for their antibacterial activity against Gram-positive bacteria namely, Staphylococcus aureus MTCC 96, Bacillus subtilis MTCC 121 and two Gram-negative bacteria namely, Escherichia coli MTCC 1652 and Pseudomonas aeruginosa MTCC 741. All the five complexes were also tested against three pathogenic fungal strains namely, Aspergillus niger, A. flavus and Penicillium sp.


Author(s):  
Bratko Filipič ◽  
Lidija Gradišnik ◽  
Adriana Pereyra ◽  
Hrvoje Mazija

ABSTRACT. The immunotherapies, as a modern therapeutic approach, get an attention because of theirs’ promise to treat a large number of different medical disorders. Immunomodulation effects of low titres (10 HA/ml) of NDV (Newcastle Disease Virus) ZG1999HDS or La Sota were tested on TLT (Human macrophage cell line) bound to PBMC (Peripheral Blood Mononuclear Cells). During the immunomodulation, the amount of NO, H2O2, lysozym and induced antibacterial activity against Gram - positive bacteria (Staphylococcus aureus, MRSA, Streptococcus pyogenes, Streptococcus agalactiae and Streptococcus mutants) and against Gram - negative bacteria (Escherichia coli, Pseudomonas aeruginosa, Proteus mirabilis and Acinetobacter baumanii) were analysed. In addition, the cytokine secretion, IL-1α, IL-2, IL-4, GM-CSF, TNF-α, IFN-α and IFN-α were evaluated. Firstly, the TLT cells are activated through the NDV ZG1999HDS or La Sota binding, followed by the NO “burst” and H2O2 and lysozyme level increase. Secondly, after the binding to the TLT cells and interaction with the PBMCs, the decrease of GM-CSF, and an increase of TNF – α and IFN – γ were found. Simultaneously, the decrease of pro – inflammatory cytokine IFN-α and the differentially increase of IL-1α, IL-2 and IL-4 were recorded. During the induction of the antibacterial response, against Gram - positive bacteria (Staphylococcus aureus, MRSA, Streptococcus pyogenes, Streptococcus agalactiae and Streptococcus mutants) the effect was one third higher with NDV ZG1999HDS compared to La Sota. Antibacterial response against Gram - negative bacteria (Escherichia coli, Pseudomonas aeruginosa, Proteus mirabilis and Acinetobacter baumanii) was not so clear. In general, NDV ZG1999HDS or La Sota activated TLT cells, further bound to PBMC; the ZG1999HDS is stronger immunomodulator than La Sota.


1988 ◽  
Vol 55 (4) ◽  
pp. 597-602 ◽  
Author(s):  
Lydia Bautista ◽  
Rohan G. Kroll

SummaryEffects of the addition of a proteinase (Neutrase 1–5S) and a peptidase (aminopeptidase DP-102) as agents for accelerating the ripening of Cheddar cheese on the survival of some non-starter bacteria (Staphylococcus aureus, Enterococcus faecalis, Escherichia coliand aSalmonellasp.) were studied throughout a 4-month ripening period. The enzymes were found to have no significant effect on the survival of the Gram-positive bacteria but some significant effects were observed, at some stages of the ripening period, with the Gram-negative bacteria in that lower levels were recovered from cheeses treated with the enzyme system.


2012 ◽  
Vol 3 ◽  
pp. 684-691 ◽  
Author(s):  
Mayuree Jaisai ◽  
Sunandan Baruah ◽  
Joydeep Dutta

Paper with antimicrobial properties was developed through in situ growth of ZnO nanorods. The targeted application for this type of paper is in health centers as wallpaper, writing paper, facemasks, tissue paper, etc. The paper was tested on three model microbes, Gram-positive bacteriaStaphylococcus aureus,Gram-negative bacteriaEscherichia coliand common airborne fungusAspergillus niger. No viable bacterial colonies or fungal spores could be detected in the areas surrounding test samples of the antimicrobial paper. Gram-negative bacteriaEscherichia coliwere found to be inhibited in an area that is 239% and 163% the area of the paper sample under different room lighting conditions, i.e., halogen and fluorescent lamp illumination, respectively. For Gram-positive bacteriaStaphylococcus aureusthe zones of inhibition surrounding the paper samples are 102% and 70%, and forAspergillus niger, 224% and 183% of the sample area, under similar lighting conditions.


2011 ◽  
Vol 322 ◽  
pp. 160-163
Author(s):  
Yin Lu ◽  
Hong Chen

A medicinal wild kiwi in China, Actinidia valvata Dunn, has been well known for its activities against leprosy and cancers. The compositions and the antimicrobial activity of its leaf oil were reported for the first time. The oil obtained by hydrodistillation and analyzed by GC and GC-MS, was characterized by the high content of monoterpenes. Linalool (48.14%) is the major component identified, followed by 1,2-dimethyl-lindoline (7.94%), linolenic acid methylester (6.57%) and (E)-phytol (5.29%). The antimicrobial activity of the oil was evaluated against four bacterial and three fungal species. The results showed that it exhibited a mild antibacterial activity against two Gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis), a significant activity against Gram-negative bacteria (Escherichia coli), and no activity on Pseudomonas aeruginosa. The test fungi were more sensitive to the oil, with a MIC range of 0.78~1.56 μL/mL than bacteria in the range which were significantly higher from 0.78 to 25.50 μL/mL.


Author(s):  
I. M. Uneze ◽  
J. O. Otonko ◽  
A. K. Adigun ◽  
S. J. Adebayo

The synthesis and application of nanoparticles is an important area of research that is gaining attention recently. In this recent project, we report the synthesis of silver nanoparticles, AgNP using aqueous solution of silver nitrate and Gnetum africanum leaf extract (reducing agent). The synthesis of AgNP was achieved by mixing aqueous solution of silver nitrate (70ml, 15.75mM) with a solution of Gnetum africanum leaf extract 100 ml) in a reaction flask and allowed to stand for 24 hours in a dark cupboard. A color change from light brown to yellowish brown was observed which indicated that synthesis of silver nanoparticles took place. The presence of AgNP was ascertained using UV-vis spectra analysis and absorption at 442 nm showed the presence of AgNP. The antioxidant assay of both the synthesized AgNP and the leaf extract was determined using DPPH. Antimicrobial activity was conducted using three different organisms which were Staphylococcus aureus, Escherichia coli and Pseudomonas respectively. The antioxidant results using DPPH scavenging ability of AgNp showed that at concentrations of 2mg/ml,1mg/ml and 0.1mg/ml, the percentage inhibition  of  DPPH  by AgNp was 61.69, 53.06 and 38.31 respectively and that of Gnetum africanum leaf extract was 81.32, 78.49, and 58.29 respectively at the same concentrations using Ascorbic acid as a standard. The antimicrobial activity of both the synthesized AgNps and Gnetum Africanum Leaf extract using one gram positive bacteria (Staphylococcus aureus) and two gram negative bacteria (Escherichia coli and Pseudomonas) revealed that the synthesized AgNps showed lesser activity than Gnetumafricanum leaf extract for both the gram positive bacteria (Staphylococcus aureus) and gram negative bacteria (Pseudomonas) and (Escherichia coli). From the above findings, it can be observed that Gnetum Africanum Leaf extract reduced Ag+ to Ag0 and also both the synthesized AgNps and the Gnetum Africanum Leaf extract showed reasonable antioxidant activity against DPPH and antimicrobial activity against the tested microorganisms. This implied that both samples have medicinal values.


Author(s):  
Adnal K. P. Husein Putra ◽  
Sri Sundari

Background: This study provides an overview of diabetic ulcer infection, antibiotic susceptibility patterns, the most common types of antibiotics, factors influence in antibiotics administrations, and verifying the guideline used of antibiotics.Methods: The research used descriptive analysis combined with interviews. The study was starting from February-March 2021. Eighty-six diabetic ulcer patients were selected considering the inclusion and exclusion criteria. We interviewed seven doctors.Results: 71 bacterias were found with a gram-negative bacteria count of 80.3%- higher than gram-positive bacteria (19.7%). The most common gram-negative bacteria found are Escherichia coli (12.7%) and show the most heightened sensitivity with imipenem (80.7%), while cefuroxime and trimethoprim-sulfamethoxazole show the highest resistance (64.9%). The most common gram-positive bacteria found are Staphylococcus aureus (14.1%), and vancomycin shows the most heightened sensitivity (100%), while penicillin shows the highest resistance (71.4%). The most common single antibiotic administration was ceftriaxone, as well as a combination of two antibiotics, namely ceftriaxone and metronidazole.Conclusions: Escherichia coli was the most gram-negative bacteria, which has the highest sensitivity with imipenem, while Staphylococcus aureus was the most gram-positive bacteria, which has the most heightened sensitivity with vancomycin. The most common single antibiotic administration was ceftriaxone, as well as a combination of two antibiotics, ceftriaxone and metronidazole. Factors that influence antibiotics administration are patient condition, susceptibility testing, training, and advice from colleagues. Every doctor uses different guidelines for diabetic foot ulcer.


Author(s):  
Satish M. Chavan

Synthesis of novel ethyl 3-amino-5-(methylthio)-4-(5-substituted phenyloxazol-2-yl) thiophene-2-carboxylate derivatives from 3-amino-4-carbamoyl-5-(methylthio)thiophene-2-carboxylate was carried out by traditional as well as microwave irradiation green protocol. Ethyl 3-amino-5-(methylthio)-4-(5-substituted phenyloxazol-2-yl) thiophene-2-carboxylate derivatives were screened for antimicrobial screening against gram positive bacteria Staphylococcus aureus (ATCC 29737), gram negative bacteria Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853) and Candida albicans (MTCC 277), Aspergillus niger (MCIM 545) fungi.


Molbank ◽  
10.3390/m1078 ◽  
2019 ◽  
Vol 2019 (3) ◽  
pp. M1078 ◽  
Author(s):  
Kazakova ◽  
Brunel ◽  
Khusnutdinova ◽  
Negrel ◽  
Giniyatullina ◽  
...  

Synthesis of A-ring-modified lupane, oleanane and ursane type triterpenoid conjugates with spermidine through an aldimine linkage or diethylentriamine via an amide bond is described. These derivatives were evaluated for their in vitro antimicrobial properties against human pathogens. Except for derivatives 1 and 7, all compounds have moderate to weak minimum inhibitory concentrations (MICs) against Gram-positive Staphylococcus aureus bacteria, with MICs varying from 3.125 to 200 µM. Compound 11 is efficient against Escherichia coli and Pseudomonas aeruginosa, with MICs of 25 and 50 µM, respectively, while all other derivatives do not possess important antimicrobial activities against these Gram-negative bacteria.


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