scholarly journals SYNTHESIS, CHARACTERIZATION AND ANTIMICROBIAL STUDIES ON CERTAIN SUBSTITUTED ARYLAZO IMIDAZOLE CONTAINING OXADIAZOLES

Author(s):  
Sreedevi MEESRAGANDA ◽  
Raghavendra Gum Prasad ALURU ◽  
Spoorthy Yadan NARASIMBA ◽  
Ravindnmath Laxmana Rao Krishna RAO

A series of novel substituted l-[5-(2-methyl-5-nitro-4phenyl-imidazol-lyl methyl)-2-phenyl-(1,3,4)oxadiazol-3-yl]-ethanones have been synthesized. Formation of 1,3,4-oxadiazole ring was accomplished by the reaction of the corresponding hydrazide with acetic anhydride. The structure determination of these compounds has been made on the basis of IR, 1H NMR, and elemental analysis. All the compounds were screened for their antibacterial activity. The antimicrobial activity of title compounds were examined against two gram-negative (Staphylococcus aureus and Bacillus subtilis), two gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa), and antifungal activity was carried out against Candida albicans. The MIC values for the newly synthesized compounds have been assessed by serial dilution method All the compounds demonstrated potent antibacterial activity.

2021 ◽  
Vol 21 (5) ◽  
pp. 2879-2891
Author(s):  
Enrico Podda ◽  
M. Carla Aragoni ◽  
Massimiliano Arca ◽  
Giulia Atzeni ◽  
Simon J. Coles ◽  
...  

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.


1969 ◽  
Vol 15 (9) ◽  
pp. 1067-1076 ◽  
Author(s):  
A. H. Amin ◽  
T. V. Subbaiah ◽  
K. M. Abbasi

Berberine sulfate was shown to possess antimicrobial activity against a wide variety of microorganisms including Gram-positive and Gram-negative bacteria, fungi, and protozoa. The antibacterial activity against Vibrio cholerae and Staphylococcus aureus was dependent on the inoculum size of the test organism and pH of the medium. A method of microbiological assay sensitive to 5–10 μg/ml of the drug was developed. The drug was shown to exert a more rapid antibacterial activity than chloramphenicol and tetracycline on V. cholerae, the K values being 2.4 ×10−2 sec−1, 7.8 × 10−3 sec−1, and 5.2 × 10−3 sec−1 respectively. Berberine sulfate was shown to be bacteriocidal to V. cholerae and bacteriostatic to S. aureus, at concentrations of 35 and 50 μg/ml. In both these organisms concentrations of 35 and 50 μg/ml of the drug inhibited ribonucleic acid (RNA) and protein synthesis almost immediately after the addition of the drug. There was little effect on deoxyribonucleic acid (DNA) synthesis at these concentrations.


Molecules ◽  
2020 ◽  
Vol 25 (10) ◽  
pp. 2374
Author(s):  
Paula C. Alves ◽  
Patrícia Rijo ◽  
Catarina Bravo ◽  
Alexandra M. M. Antunes ◽  
Vânia André

We report herein three novel complexes whose design was based on the approach that consists of combining commercially available antibiotics with metals to attain different physicochemical properties and promote antimicrobial activity. Thus, new isostructural three-dimensional (3D) hydrogen bonding frameworks of pipemidic acid with manganese (II), zinc (II) and calcium (II) have been synthesised by mechanochemistry and are stable under shelf conditions. Notably, the antimicrobial activity of the compounds is maintained or even increased; in particular, the activity of the complexes is augmented against Escherichia coli, a representative of Gram-negative bacteria that have emerged as a major concern in drug resistance. Moreover, the synthesised compounds display similar general toxicity (Artemia salina model) levels to the original antibiotic, pipemidic acid. The increased antibacterial activity of the synthesised compounds, together with their appropriate toxicity levels, are promising outcomes.


2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Paulina L. Páez ◽  
Claudia M. Bazán ◽  
María E. Bongiovanni ◽  
Judith Toneatto ◽  
Inés Albesa ◽  
...  

The prevalence of antibiotic resistance has resulted in the need for new approaches to be developed to combat previously easily treatable infections. The main aim of this work was to establish the potential of the syntheticα-diimine chromium(III) and ruthenium(II) complexes (where theα-diimine ligands are bpy = 2,2-bipyridine, phen = 1,10-phenanthroline, and dppz = dipyrido[3,2-a:2′,3′-c]-phenazine) like [Cr(phen)3]3+, [Cr(phen)2(dppz)]3+, [Ru(phen)3]2+, and [Ru(bpy)3]2+as antibacterial agents by generating oxidative stress. The [Cr(phen)3]3+and [Cr(phen)2(dppz)]3+complexes showed activity against Gram positive and Gram negative bacteria with minimum inhibitory concentrations (MICs) ranging from 0.125 μg/mL to 1 μg/mL, while [Ru(phen)3]2+and [Ru(bpy)3]2+do not exhibit antimicrobial activity against the two bacterial genera studied at the concentration range used. When ciprofloxacin was combined with [Cr(phen)3]3+for the inhibition ofStaphylococcus aureusandEscherichia coli, an important synergistic effect was observed, FIC 0.066 forS. aureusand FIC 0.064 forE. coli. The work described here shows that chromium(III) complexes are bactericidal forS. aureusandE. coli. Our results indicate thatα-diimine chromium(III) complexes may be interesting to open new paths for metallodrug chemotherapy against different bacterial genera since some of these complexes have been found to exhibit remarkable antibacterial activities.


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.


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.


2011 ◽  
Vol 6 (5) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Janne Rojas ◽  
Alexis Buitrago ◽  
Luis Rojas ◽  
Antonio Morales ◽  
María Lucena ◽  
...  

The essential oil from the fruits of Vismia baccifera Triana & Planch. (Gutttiferae), collected in June 2009, was analyzed by GC/MS. A yield of 0.6% oil was obtained by hydrodistillation. Twenty-seven components were identified by comparison of their mass spectra with those in the Wiley GC-MS Library data base. The major components were trans-cadin-1,4-diene (36.6%), cis-cadin-1,4-diene (18.8%) and β-caryophyllene (11.9%). The essential oil showed a broad spectrum of antibacterial activity against the important human pathogenic Gram-positive and Gram-negative bacteria Staphylococcus aureus (ATCC 25923), Enterococcus faecalis (ATCC 29212), Escherichia coli (ATCC 25992), Pseudomonas aeruginosa (ATCC 27853) and Klebsiella pneumoniae (ATCC 23357) with MIC values ranging from 9 to 37 μg/mL.


1999 ◽  
Vol 67 (8) ◽  
pp. 4106-4111 ◽  
Author(s):  
Olga Shamova ◽  
Kim A. Brogden ◽  
Chengquan Zhao ◽  
Tung Nguyen ◽  
Vladimir N. Kokryakov ◽  
...  

ABSTRACT We purified three proline-rich antimicrobial peptides from elastase-treated extracts of sheep and goat leukocytes and subjected two of them, OaBac5α and ChBac5, to detailed analysis. OaBac5α and ChBac5 were homologous to each other and to bovine Bac5. Both exhibited potent, broad-spectrum antimicrobial activity under low-concentration salt conditions. While the peptides remained active againstEscherichia coli, Pseudomonas aeruginosa,Bacillus subtilis, and Listeria monocytogenesin 100 mM NaCl, they lost activity against Staphylococcus aureus and Candida albicans under these conditions. ChBac5 was shown to bind lipopolysaccharide, a property that could enhance its ability to kill gram-negative bacteria. Proline-rich Bac5 peptides are highly conserved in ruminants and may contribute significantly to their innate host defense mechanisms.


2021 ◽  
Vol 33 (11) ◽  
pp. 2662-2666
Author(s):  
Amnuay Noypha ◽  
Paweena Porrawatkul ◽  
Nongyao Teppaya ◽  
Parintip Rattanaburi ◽  
Saksit Chanthai ◽  
...  

Borassus flabellifer vinegar–graphene quantum dots (BFV-GQDs) were successfully synthesized using a pyrolysis method with Borassus flabellifer vinegar (BFV) as the precursor. All the samples were characterized using ultraviolet-visible spectrophotometry (UV-Vis), scanning electron microscopy (SEM) and energy-dispersive X-ray spectroscopy (EDX). The antibacterial activities of BFV-GQDs against strains of Gram-negative bacteria (Escherichia coli) and Gram-positive bacteria (Staphylococcus aureus) were determined using the agar well diffusion method for preliminary screening, while minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were determined using the broth macro-dilution method. The zones of inhibition were compared with those of citric acid–graphene quantum dots (CA-GQDs). It was observed that the synthesized BFV-GQDs demonstrated excellent antibacterial activity against Staphylococcus aureus (82.3%) and good antibacterial activity against Escherichia coli (73.3%). The MIC of BFV-GQDs against E. coli was 6.25 mg/mL and S. aureus was 12.5 mg/mL, whereas the MBC of BFV-GQDs against E. coli was 12.5 mg/mL and S. aureus was 25.0 mg/mL.


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