scholarly journals Ferrocene-Derived Pyrazinoyl and Nicotinoyl Schiff-Bases: Their Synthesis, Characterization and Biological Properties

1999 ◽  
Vol 6 (3) ◽  
pp. 149-152 ◽  
Author(s):  
Zahid H. Chohan ◽  
M. Praveen

A novel class of acetylferrocene-derived Schiff-bases such as 2-pyrazinoyl-1-(2-ferroceneylmethylene)- hydrazide (HL1) and 2-nicotinoyl-1-(2-ferrocenylmethylene)hydrazide (HL2) have been synthesized and characterized by their IR, H1 NMR, C13 NMR and microanalytical date. The biological effect induced due to the coupling of ferrocene molecule with the aroylhydrazines e.g., pyrazinoylhydrazine and nicotinoylhydrazine has been studied against bacterial species such as Escherichia coli, Pseudomonas aeruginosa , Staphylococcus aureus and Klebsiella pneumonae.

1998 ◽  
Vol 5 (5) ◽  
pp. 267-274 ◽  
Author(s):  
Zahid H. Chohan ◽  
Marapaka Praveen ◽  
Syed K. A. Sherazi

Biologically active complexes of Co(II), Ni(II), Cu(II) and Zn(II) with novel ONO, NNO and SNO donor pyrazinoylhydrazine-derived compounds have been prepared and characterized on the basis of analytical data and various physicochemical studies. Distorted octahedral structures for all the complexes have been proposed. The synthesized ligands and their complexes have been screened for their antibacterial activity against bacterial species Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Klebsiella pneumonae. The activity data show the metal complexes to be more active than the parent free ligands against one or more bacterial species.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1740
Author(s):  
Elena Trizna ◽  
Diana Baidamshina ◽  
Anna Gorshkova ◽  
Valentin Drucker ◽  
Mikhail Bogachev ◽  
...  

While in a biofilm, bacteria are extremely resistant to both antimicrobials and the immune system, leading to the development of chronic infection. Here, we show that bovine hyaluronidase fused with a copolymer of 1,4-ethylenepiperazine N-oxide and (N-carboxymethyl) -1,4-ethylenepiperazinium bromide (Longidaza®) destroys both mono- and dual-species biofilms formed by various bacteria. After 4 h of treatment with 750 units of the enzyme, the residual biofilms of Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa and Klebsiella pneumoniae preserved about 50–70% of their initial mass. Biomasses of dual-species biofilms formed by S. aureus and the four latter species were reduced 1.5-fold after 24 h treatment, while the significant destruction of S. aureus–P. aeruginosa and S. aureus–K. pneumoniae was also observed after 4 h of treatment with Longidaza®. Furthermore, when applied in combination, Longidaza® increased the efficacy of various antimicrobials against biofilm-embedded bacteria, although with various increase-factor values depending on both the bacterial species and antimicrobials chosen. Taken together, our data indicate that Longidaza® destroys the biofilm structure, facilitating the penetration of antimicrobials through the biofilm, and in this way improving their efficacy, lowering the required dose and thus also potentially reducing the associated side effects.


2019 ◽  
Vol 85 (9) ◽  
Author(s):  
A. Jochim ◽  
T. Shi ◽  
D. Belikova ◽  
S. Schwarz ◽  
A. Peschel ◽  
...  

ABSTRACTMultidrug-resistant bacterial pathogens are becoming increasingly prevalent, and novel strategies to treat bacterial infections caused by these organisms are desperately needed. Bacterial central metabolism is crucial for catabolic processes and provides precursors for anabolic pathways, such as the biosynthesis of essential biomolecules like amino acids or vitamins. However, most essential pathways are not regarded as good targets for antibiotic therapy since their products might be acquired from the environment. This issue raises doubts about the essentiality of such targets during infection. A putative target in bacterial anabolism is the methionine biosynthesis pathway. In contrast to humans, almost all bacteria carry methionine biosynthesis pathways which have often been suggested as putative targets for novel anti-infectives. While the growth of methionine auxotrophic strains can be stimulated by exogenous methionine, the extracellular concentrations required by most bacterial species are unknown. Furthermore, several phenotypic characteristics of methionine auxotrophs are only partly reversed by exogenous methionine. We investigated methionine auxotrophic mutants ofStaphylococcus aureus,Pseudomonas aeruginosa, andEscherichia coli(all differing in methionine biosynthesis enzymes) and found that each needed concentrations of exogenous methionine far exceeding that reported for human serum (∼30 µM). Accordingly, these methionine auxotrophs showed a reduced ability to proliferate in human serum. Additionally,S. aureusandP. aeruginosamethionine auxotrophs were significantly impaired in their ability to form and maintain biofilms. Altogether, our data show intrinsic defects of methionine auxotrophs. This result suggests that the pathway should be considered for further studies validating the therapeutic potential of inhibitors.IMPORTANCENew antibiotics that attack novel targets are needed to circumvent widespread resistance to conventional drugs. Bacterial anabolic pathways, such as the enzymes for biosynthesis of the essential amino acid methionine, have been proposed as potential targets. However, the eligibility of enzymes in these pathways as drug targets is unclear because metabolites might be acquired from the environment to overcome inhibition. We investigated the nutritional needs of methionine auxotrophs of the pathogensStaphylococcus aureus,Pseudomonas aeruginosa, andEscherichia coli. We found that each auxotrophic strain retained a growth disadvantage at methionine concentrations mimicking those availablein vivoand showed that biofilm biomass was strongly influenced by endogenous methionine biosynthesis. Our experiments suggest that inhibition of the methionine biosynthesis pathway has deleterious effects even in the presence of external methionine. Therefore, additional efforts to validate the effects of methionine biosynthesis inhibitorsin vivoare warranted.


2000 ◽  
Vol 7 (3) ◽  
pp. 133-139 ◽  
Author(s):  
Zahid H. Chohan ◽  
M. A. Farooq ◽  
M. S. Iqbal

Some acylhydrazine derived ONO donor Schiff bases and their Co(II) and Ni(II) complexes have been prepared having the same metal ion (cation) but different anions. These synthesized metal(II) complexes have been characterized on the basis of their elemental analyses, magnetic moment, molar conductance, and IR and electronic spectral data. All of the Schiff base ligands function as tridentates and the deprotonated enolic form is preferred for coordination. In order to evaluate the effect of anions on the bactericidal activity, these synthesized complexes, in comparison to the uncomplexed Schiff bases have been screened against bacterial species., Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa and the results are reported.


2020 ◽  
Vol 71 (1) ◽  
pp. 244-248
Author(s):  
Gladiola Tantaru ◽  
Mihai Apostu ◽  
Cristina Mihaela Ghiciuc ◽  
Antonia Poiata ◽  
Alina Stefanache ◽  
...  

The article presents some bis-Schiff bases - halogenated derivatives of ortho-hydroxy-ketones - with great potential for antimicrobial and antiinflammatory activity. The antimicrobial activities of the Schiff bases were tested in comparison with Chloramphenicol, Nystatin, and Ampicillin upon the following strains: Staphylococcus aureus (ATCC 25923), Sarcina lutea (ATCC 9341), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853), Candida albicans (ATCC 1023), Candida glabrata, two Staphylococcus aureus strains, and several clinical isolates (Proteus mirabilis, Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae). Those compounds were found to be active against Gram-positive or Gram-negative bacteria, and had an anti-inflammatory effect comparable to that of Indomethacin.


Author(s):  
Immaculata U. Nwankwo ◽  
Kelechi C. Edward ◽  
Chinedu N. Nwoba ◽  
Chinyere V. Okwudiri

Introduction: The skin is a barrier that limits invasion and growth of pathogenic bacteria. Bacterial species in patients with skin infection and their antibiogram were evaluated for the presence of inhabiting bacteria. Method: The sample obtained with swab sticks were streaked on their respective culture plates containing nutrient agar, MacConkey agar and blood agar, incubated 370 for 24h. The recovered bacteria after incubation were characterized and identified according to standard microbiological criteria. Results: Five bacteria species were isolated which includes Staphylococus aureus; Escherichia coli, Klebsiella specie, Proteus sp and Pseudomonas aeruginosa. Staphylococus aureus (33.03%) had the highest percentage occurrence while Proteus Sp (9.17%) had the lowest percentage occurrence. The highest number of isolates were recovered from male patients (61.47%). Age wise the least percentage of isolates were gotten from age group 31-40 (1.83%) while the highest was obtained from those within the age range of 11-20 (40.37%) followed by 1-10 years of age (25.69%). More isolates were recovered from in-patients (68.81%) than from Out-patients (31.19%). The antibiotic sensitivity test showed that Klebsiella sp, Proteus spp and Staphylococcus aureus were sensitivity to all the antibiotics tested while pseudomonas aeruginosa had 30% activity (sensitivity to only 3 drugs) for the antibiotics used in this study. Conclusion: From this study, it can be said that Staphylococcus aureus, Escherichia coli, Klebsiella sp, Proteus sp and Pseudomonas aeruginosa are implicated in the skin infections in humans and their presence if not treated will lead to long term disease in human affected.


1997 ◽  
Vol 4 (5) ◽  
pp. 267-272 ◽  
Author(s):  
Zahid H. Chohan ◽  
M. Praveen ◽  
A. Ghaffar

Biologically active tridentate amino acid (Alanine, Glycine & Tyrosine) derived Schiff-bases and their Co(II), Cu(II) & Ni(II) complexes have been synthesised and characterised on the basis of their conductance and magnetic measurements, elemental analysis and C13-NMR, H1-NMR, IR and electronic spectral data. These Schiff-bases and their complexes have been evaluated for their antibacterial activity against bacterial species such as Staphylococcus aureus, Escherichia coli, Klebsiella pneumonae, Proteus vulgarus and Pseudomonas aeruginosa and this activity data show the metal complexes to be more antibacterial than the Schiff-bases against one or more bacterial species.


2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Dereje Nigussie ◽  
Gail Davey ◽  
Belete Adefris Legesse ◽  
Abebaw Fekadu ◽  
Eyasu Makonnen

Abstract Background Patients with lymphoedema are at high risk of getting bacterial and fungal wound infections leading to acute inflammatory episodes associated with cellulitis and erysipelas. In Ethiopia, wound infections are traditionally treated with medicinal plants. Methods Agar well diffusion and colorimetric microdilution methods were used to determine the antibacterial activity of methanol extracts of the three medicinal plants against Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, Shewanella alage, methicillin-resistant S. aureus ATCC®43300TM, Staphylococcus aureus ATCC25923, Escherichia coli ATCC25922, Klebsiella pneumoniae ATCC700603, and Pseudomonas aeruginosa ATCC37853. Results The methanol extract of L. inermis leaves showed high activity against all tested bacterial species, which was comparable to the standard drugs. Similarly, the extracts of A. indica showed activity against all tested species though at higher concentrations, and higher activity was recorded against Streptococcus pyogenes isolates at all concentrations. However, the extract of A. aspera showed the lowest activity against all tested species except Streptococcus pyogenes isolates. The lowest minimum inhibitory concentration (MIC) was recorded with the extract of L. inermis against E. coli isolate and S. aureus ATCC 25923. Conclusion Methanol extracts of L. inermis, A. indica, and A. aspera leaves exhibited antimicrobial activity against selected bacterial isolates involved in wound infections, of which the methanol extracts of L. inermis exhibited the highest activity. The results of the present study support the traditional use of plants against microbial infections, which could potentially be exploited for the treatment of wound infections associated with lymphoedema.


Author(s):  
Mohammad Farooq Bhutta ◽  
Ashfaq Hussain ◽  
Salman Baig ◽  
Asad Ullah ◽  
Sarwath Fatimee ◽  
...  

Aim: To find out the frequency of different bacterial species and their antibiogram among the patients of chronic suppurative otitis media. Study Design: Descriptivecross-sectional. Place and Duration of Study: The study was conducted at the ENT department of Bahawal Victoria hospital between July to December 2020. Methodology: About 50 patients presented with unilateral or bilateral ear discharge and diagnosed as a case of chronic suppurative otitis media were included in the study. The disk diffusion method was used on Mueller-Hinton Agar to detect antimicrobial susceptibility. Multipledrugs were tested for checking antimicrobial susceptibility. The data were analyzed by using Statistical Package for the Social Sciences (SPSS) version 20. Results: The mean age of the study participants was 13.89 ± 12.37 years. The majority of participants were froma younger age group i.e. less than10 years of age with female predominance. It had been found that the majority of cases (51%) were having Staphylococcus aureus infestation followed by Pseudomonas aeruginosa, Escherichia coli and very few with Proteus mirabilis. On the other hand, multiple drugs were tested to find out the antimicrobial susceptibility among the cases of chronic otitis media and the results reported that all the bacterial species were susceptible to Ceftriaxone while the other antibiotics were havinga variable response for different strains of bacteria. Conclusion: Results concluded that the Staphylococcus aureus was the most common organism followed by Pseudomonas aeruginosa, Escherichia coli and very few with Proteus mirabilis. It is important to identify the pathogenic organism and its sensitivity pattern before prescribing any antibiotic.


2001 ◽  
Vol 8 (2) ◽  
pp. 95-101 ◽  
Author(s):  
Zahid H. Chohan ◽  
Maimoon F. Jaffery ◽  
Claudiu T. Supuran

Schiff bases were obtained by condensation of 2-amino-l,3,4-thiadiazole with 5-substituted-salicylaldehydes which were further used to obtain complexes of the type [M(L)2]Cl2, where M=Co(II), Cu(II), Ni(II) or Zn(II). The new compounds described here have been characterized by physical, spectral and analytical data, and have been screened for antibacterial activity against several bacterial strains such as Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa. The antibacterial potency of these Schiff bases increased upon chelation/complexation, against the tested bacterial species, opening new aproaches in the fight against antibiotic resistant strains.


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