scholarly journals Novel 4-Thiazolidinone Derivatives as Anti-Infective Agents: Synthesis, Characterization, and Antimicrobial Evaluation

2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
Amit Gupta ◽  
Rajendra Singh ◽  
Pankaj K. Sonar ◽  
Shailendra K. Saraf

A series of new 4-thiazolidinone derivatives was synthesized, characterized by spectral techniques, and screened for antimicrobial activity. All the compounds were evaluated against five Gram-positive bacteria, two Gram-negative bacteria, and two fungi, at concentrations of 50, 100, 200, 400, 800, and 1600 µg/mL, respectively. Minimum inhibitory concentrations of all the compounds were also determined and were found to be in the range of 100–400 µg/mL. All the compounds showed moderate-to-good antimicrobial activity. Compounds4a[2-(4-fluoro-phenyl)-3-(4-methyl-5,6,7,8-tetrahydro-quinazolin-2-yl)-thiazolidin-4-one] and4e[3-(4,6-dimethyl-pyrimidin-2-yl)-2-(2-methoxy-phenyl)-thiazolidin-4-one] were the most potent compounds of the series, exhibiting marked antimicrobial activity againstPseudomonas fluorescens,Staphylococcus aureus,and the fungal strains. Thus, on the basis of results obtained, it may be concluded that synthesized compounds exhibit a broad spectrum of antimicrobial activity.

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.


2014 ◽  
Vol 69 (9-10) ◽  
pp. 368-374 ◽  
Author(s):  
Mustafa Arisoy ◽  
Ozlem Temiz-Arpaci ◽  
Fatma Kaynak-Onurdag ◽  
Selda Ozgen

Abstract series of 2-(p-substituted phenyl)-5-(2-{4-[(p-chloro-fluorophenyl)=phenyl] piperazin-1-yl}- acetamido)-benzoxazoles were synthesized and tested for their antimicrobial activities. The structures of the new derivatives were elucidated by spectral techniques. The minimum inhibitory concentrations (MIC) of the new benzoxazoles, along with those of previously synthesized analogues, were determined against standard bacterial and fungal strains and drug-resistant isolates, and compared with those of several reference drugs. The new benzoxazole derivatives were found to possess a broad spectrum of antimicrobial activity with MIC values of 32 - 1024 μg/ml. Although the standard drugs were more active against the tested pathogens, the activities of the new benzoxazoles and the reference drugs were largely similar against the drug-resistant isolates.


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.


2019 ◽  
Vol 4 (1) ◽  
pp. 32-35
Author(s):  
Priyanka Sharma

8-Substituted-2,5-dihydro-1,5-benzothiazepine derivatives have been synthesized by the reaction of 1-(2-furyl)-3-(3,4-dimethoxyphenyl)-2-propenone with six 5-substiuted-2-minobenzenethiols in dry ethanol saturated with dry HCl gas and also in the presence of aluminium nitrate as catalyst in dry ethanol. All the newly synthesized compounds were characterized by analytical and spectral data comprising IR, 1H NMR, 13C NMR, 19F NMR and mass studies. All these compounds have also been evaluated for their antimicrobial assay against the Gram-positive bacteria, Staphylococcus aureus and the Gram-negative bacteria, Pseudomonas aeruginosa and the fungus, Candida albicans. The antifungal activity was found to be more significant than antibacterial activity.


Author(s):  
Shipra Baluja ◽  
Sumitra Chanda ◽  
Paras Ramavat

A series of oxadiazole derivatives were synthesized and were characterized by IR, 1H NMR and mass spectroscopy. All these synthesized compounds were tested for in vitro antimicrobial against four Gram positive bacteria, four Gram negative bacteria and four fungal strains in DMSO and DMF.


2021 ◽  
Vol 6 (3) ◽  
pp. 235-242
Author(s):  
Bhoomi M. Makwana ◽  
Yogesh T. Naliapara

Copper(I)-catalyzed azide alkyne cycloaddition (CuAAC) methodology to develop a library of 3-methyl quinoxaline-1,2,3-triazole hybrid molecules. The designed molecules were synthesized via efficient and purification free method. The structures of the achieved compounds were recognized based on their spectral data. The antimicrobial activity for the synthesized compounds was evaluated against four bacterial species and two fungal strains. Six compounds are broad spectrum molecule, which can inhibit the growth of both Gram-positive and Gram-negative bacteria. Two molecules show mainly antifungal activity. Compound 6e shows highest antibacterial as well as antifungal activity.


2019 ◽  
Vol 2019 ◽  
pp. 1-10
Author(s):  
Mashooq Ahmad Bhat ◽  
Mohamed A. Al-Omar ◽  
Ahmed M. Naglah ◽  
Abdul Arif Khan

A series of pyrazoles derived from the substituted enaminones were synthesized and were evaluated for antimicrobial activity. All the compounds were characterized by the spectral data and elemental analysis. The synthesized compounds were initially screened for their antimicrobial activity against ATCC 6538, NCTC 10400, NCTC 10418, and ATCC 27853. During initial screening, compounds (P1, P6, and P11) presented significant antimicrobial activity through disc diffusion assay. These compounds were further evaluated for antimicrobial activity at different time points against Gram-positive and Gram-negative bacteria and presented significant activity for 6 hours. The activity was found to be greater against Gram-positive bacteria. In contrast at 24 hours, the activity was found only against Gram-positive bacteria except compound (P11), showing activity against both types of bacteria. Compound (P11) was found to have highest activity against both Gram-positive and Gram-negative bacteria.


2021 ◽  
Vol 2 (2) ◽  
Author(s):  
Eti Nurwening Sholikhah ◽  
Maulina Diah ◽  
Mustofa ◽  
Masriani ◽  
Susi Iravati ◽  
...  

Pycnarrhena cauliflora (Miers.) Diels., local name sengkubak, is one of indigenous plants from West Kalimantan that has been used as natural flavor. Pycnorrhena cauliflora is one of species of Menispermaceae family which is rich in bisbenzylisoquinoline alkaloids. This alkaloids are known to have various biological activities including antiprotozoal, antiplasmodial, antifungal and antibacterial activities. This study aimed to investigate antimicrobial activity of  the P. cauliflora (Miers.) Diels. methanolic extracts against gram-positive and gram-negative bacteria. The methanolic extract of P. cauliflora (Miers.) Diels., root, leaf and stem were prepared by maceration. The disk-diffusion method was then used to determine the antimicrobial activity of the extracts against Streptococcus pyogenes, S. mutants, Staphylococcus aureus, S. epidermidis, Salmonella typhi, Shigella flexneri, Pseudomonas aeruginosa and Escherichia coli after 18-24 h incubation at 37 oC. Amoxicillin was used as positive control for gram-positive bacteria and ciprofloxacin was used as gram-negative bacteria. The inhibition zones were then measured in mm. Analysis were conducted in duplicates. The results showed in general the methanolic extracts of P. cauliflora (Miers.) Diels. root (inhibition zone diameter= 10-23 mm) were more active than that leaf (0-15 mm) and stem (0-17 mm) extracts against gram-positive bacteria. The zone inhibition diameter of amoxicillin as positive control was 8-42 mm. In addition, the methanolic extracts of P. cauliflora (Miers.) Diels. root (12-17 mm) were also more active than that leaf (0-12 mm) and stem (0-12 mm) extracts against gram-negative bacteria. The zone inhibition diameter of ciprofloxacin as positive control was 33-36 mm. In conclusion, the methanolic extract of P. caulifloria (Miers.) Diels. root is the most extract active against both gram-positive and gram-negative bacteria. Further study will be focused to isolate active compounds in the methanolic extract of the root.


2020 ◽  
Vol 7 (8) ◽  
pp. 1290
Author(s):  
Saswat Subhankar ◽  
K. Madhuri ◽  
Vivek D. Alone

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.


2014 ◽  
Vol 8 (3) ◽  
pp. 40-45
Author(s):  
Zina Hashem Shehab ◽  
Huda Suhail Abid ◽  
Sumaya Fadhil Hamad ◽  
Sara Haitham

The study was conducted to evaluate the inhibitory activity of methanol extract of Gardenia jasminoides leaves compared with leaf crude extracts for some organic solvents namely Methanol, Ethanol, Petroleum ether, Asetone and Chloroform on growth of some pathogenic bacteria and yeast, which included four gram positive isolates Staphylococcus aureus, Enterococcus faecalis, Streptococcus pyogenes and Bacillus cereus and gram negative isolates Escherichia coli, Salmonella typhi, Proteus vulgaris and Pseudomonas aeruginosa and some yeasts Candida albicans and Saccharomyces boulardii, by using well diffusion method. The inhibitory activity of extracts in the tested bacterial strains and yeasts was varied according to the type of extracting solvents and are tested microorganisms. The methanol callus extract which grown on Murashige and Skoog (MS) media by using (Naphthalen acitic acid) NAA and (Benzyle adenine) BA as growth regulator highly effective as compared to the other extracts as for inhibition of three gram positive bacteria and three gram negative bacteria,which include Staphylococcus aureus and, Proteus vulgaris, followed by acetone and ethanolic extracts which include two gram positive bacteria and two gram negative bacteria. All extracts had highly effect in growth of Candida albicans while all crude extracts didn’t show any sensitivity against Saccharomyces boulardii, and when we’d done (High Performance Liquid Chromatography) HPLC test for detection of some active compound we found Quinic acid, Iridiods glycosides and Crocin which its rate in fresh callus was higher than fresh leaves.


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