scholarly journals Synthesis, Characterization and Biological Evaluation of Ciprofloxacin-p-nitrobenzoylated and Its Transition Metal Analogues

2019 ◽  
Vol 11 (3) ◽  
pp. 351-363
Author(s):  
M. G. Rabbani ◽  
M. R. Islam

Six novel transition metal complexes of ciprofloxacin-p-nitro benzoyl derived from ciprofloxacin have been synthesized to find out their medicinal evaluation. It has been characterized by different techniques, i.e., UV-Vis, IR, NMR and mass spectrometry together with elemental analysis and molar conductivity. All the compounds were screened for their antimicrobial activities by the disc diffusion method. Cytotoxicity was also made against brine shrimp lethality assay. The antimicrobial activity of the analogues compared with the parent was evaluated against three Gram-positive, seven Gram-negative bacterial strains and three fungi. The synthesized compounds demonstrated a variety of antibacterial profiles among which most of the analogues showed a comparable or better activity compared to the ciprofloxacin. Moreover, unlike ciprofloxacin, most of the derivatives were also found to show antifungal activity. Interestingly, all the derivatives possessed an enhanced activity in comparison to the ciprofloxacin against Candida albicans. Regarding cytotoxicity, most of the derivatives showed to a greater degree cytotoxic agent compared to ciprofloxacin.

2020 ◽  
Vol 12 (3) ◽  
pp. 349-362
Author(s):  
M. G. Rabbani ◽  
M. R. Islam

Present work includes synthesis of five NH-analogues of ciprofloxacin, 2-6 have been prepared to find out their medicinal assessment, for instance, antibacterial, antifungal, and cytotoxicity. The structure of the analogues has been confirmed by FT- IR, 1H-NMR, 13C-NMR, mass spectral data and elemental analysis. The compounds were screened for their antimicrobial activities by the disc diffusion method. Cytotoxicity was also tested against brine shrimp lethality assay. The antimicrobial activity of the analogues compared with the parent was evaluated against three Gram-positive, five Gram-negative bacterial strains and three fungi. The synthesized compounds showed diverse antimicrobial profile among which derivatives, 2 and 3 possessed enhanced activity in contrast to the ciprofloxacin. Additionally, unlike ciprofloxacin, most of the derivatives were also found to show antifungal activity against Candida albicans. Regarding cytotoxicity, most of the derivatives exhibited better cytotoxic activity than ciprofloxacin.


2011 ◽  
Vol 6 (2) ◽  
pp. 1934578X1100600
Author(s):  
Andrés F. Peralta-Bohórquez ◽  
Clara Quijano-Célis ◽  
Mauricio Gaviria ◽  
Consuelo Vanegas-López ◽  
Jorge A. Pino

The chemical composition of the volatile compounds from the leaves of Lantana canescens Kunth (Verbenaceae) and L. lopez-palacii Moldenke grown in Colombia were analyzed by GC and GC/MS. One hundred and thirty-nine volatile compounds were identified in L. canescens, of which the major ones were β-caryophyllene (13.5%), germacrene D (10.3%) and 1-octen-3-ol (8.4%). In the oil obtained from L. lopez-palacii, eighty-three compounds were identified, of which the most prominent were 1-octen-3-ol (24.4%) and β-caryophyllene (15.2%). The in vitro antibacterial activity of the L. lopez-palacii essential oil was studied against three bacterial strains using the disc diffusion method. No antimicrobial activity was found against Escherichia coli, Enterobacter sakazakii and Listeria monocytogenes.


2019 ◽  
Vol 31 (9) ◽  
pp. 1905-1912 ◽  
Author(s):  
Kummara Srinivasulu ◽  
Katreddi Hussain Reddy ◽  
K. Anuja ◽  
D. Dhanalakshmi ◽  
Golla Ramesh

Metal complexes having the composition M(Bipy)Cl2 (where, M = Cu(II), Ni(II) and Co(II); Bipy = 2,2-bipyridyl) are reacted with 2-acetylthiophene thiosemicarbazone (ATT) to produce heteroleptic transition metal complexes with molecular formula [M(Bipy)ATT]. The complexes are characterized by mass spectra, molar conductivity, infrared and electronic spectra. Electrochemical behaviour of these metal complexes was investigated by cyclic voltammetric studies. The metal complexes show quasi reversible cyclic voltammetric responses for the Cu(II)/Cu(I) couple. The binding properties of these complexes with calf-thymus DNA have been investigated by using absorption spectrophotometry. Metal complexes are screened for their antibacterial activity by using agar well diffusion method against pathogenic bacterial strains viz. Escherichia coli and Staphylococcus aureus. Antibacterial activity of the present complexes are comparable with the activity of ciprofloxacin. The Cu(Bipy)Cl2 complex inhibits bacteria more strongly than any other complex. The Ni(Bipy)ATT complex shows more activity than the parent complex, Ni(Bipy)Cl2.


2021 ◽  
Author(s):  
Julie Piron ◽  
Jessica Pastour ◽  
Niklas Tysklind ◽  
Juliette Smith-Ravin ◽  
Fabienne Priam

AbstractMarine sponges are known for their antimicrobial, antifungal, and cytotoxic activity. In this study, the activity of aqueous and ethanoic extracts of 3 sponges from Martinique were tested on 5 bacterial strains: Bascillus cereus (CIP 783), Echerichia coli (CIP 54127), Pseudomonas aeruginosa (CIP A22), Staphylococcus aureus (CIP 67.8) and Staphylococcus saprophyticus (CIP 76125). The antimicrobial activity of Agelas clathrodes, Desmapsamma anchorata, and Verongula rigida, was demonstrated using the disc diffusion method and by determining the minimum inhibitory concentration and the minimum bactericidal concentration. The ethanoic extract of Agelas clathrodes had an inhibitory activity specifically on Staphylococcus aureus and Staphylococcus saprophyticus. No activity was observed for the other extracts. Further chemical analyses will be carried out in order to identify the active molecules of these sponges.


2011 ◽  
Vol 94 (1) ◽  
pp. 243-250 ◽  
Author(s):  
Fazli Sozmen ◽  
Burcu Uysal ◽  
Birsen S Oksal ◽  
Elif Odabas Kose ◽  
I Gokhan Deniz

Abstract The components of the essential oils (EOs) obtained by solvent-free microwave extraction (SFME) and hydrodistillation (HD) from endemic Origanum saccatum P.H. Davis were identified by using GC/MS. The main constituents of both EOs obtained by SFME and HD, respectively, from O. saccatum were p-cymene (72.5 and 70.6%), thymol (9.32 and 8.11%), and carvacrol (7.18 and 6.36%). The EO obtained by SFME contained substantially higher amounts of oxygenated compounds and lower amounts of monoterpenes than did the EO obtained by HD. The antibacterial activities of the EOs obtained by SFME and HD were evaluated with the disc diffusion method by comparison with 10 different bacterial strains. The antibacterial activity of the EO extracted by SFME was found to be more effective than that of the EO extracted by HD against seven of the tested bacteria.


Author(s):  
Eleena Panda ◽  
Chinmay Pradhan ◽  
Anath Bandhu Das

<p><strong>Objective: </strong>The present study aims at the comparative analysis of phytoconstituents and antimicrobial activities of four ecotypes of Odisha, India, each of <em>Oxalis corniculata </em>L. (OC-Eco-1, OC-Eco-2, OC-Eco-3, OC-Eco-4) and <em>Oxalis debilis</em> Kunth. (OD-Eco-1, OD-Eco-2, OD-Eco-3, OD-Eco-4) of the family Oxalidaceae.</p><p><strong>Methods: </strong>The ecotypes were collected from four districts (Balasore, Bhadrak, Jajpur, Khurda) of Odisha, India. The qualitative phytochemical screening was done to test glycosides, saponins, tannins and terpenoids. Further analysis of phytochemicals was also screened through TLC and HPTLC. Antimicrobial potentiality of leaf extract of various ecotypes was studied against <em>Bacillus subtilis</em>, <em>Pseudomonas aeruginosa</em> and <em>Streptococcus epidermis</em> by disc diffusion method.</p><p><strong>Results: </strong>Tannin and terpenoids estimation revealed that significantly high amount of phytoconstituents were present in OD-Eco-3 of <em>O. debilis</em>. The methanolic leaf extracts of each ecotype were screened for qualitative analysis of phytochemical through TLC and HPTLC that showed maximum 16 compounds in <em>O. debilis </em>(OD-Eco-3)<em> </em>a new report, as compared to <em>O. corniculata. </em>All the four ecotypes of <em>O. debilis</em><em> </em>showed some new HPTLC bands (Rf 0.96, 0.90, 0.90, 0.81) as compared to <em>O. corniculata </em>that occupied 7.70%, 22.38%, 23.79% and 34.42% of peak area respectively. Cluster analysis on the basis of HPTLC banding pattern showed a close affinity among ecotypes of each species. Crude extracts showed antibacterial activity against <em>B. subtilis</em>, <em>P. aeruginosa</em> and <em>S. epidermis</em>. Leaf extracts of ecotypes of <em>O. corniculata</em> showed zones of inhibition and MIC better than that of <em>O. debilis </em>against <em>S. epidermis</em>.<strong></strong></p><p><strong>Conclusion: </strong>The findings significantly reported some new compounds for the first time in <em>O. debilis. </em>The study also indicated a promising potential of antimicrobial activity of <em>O. debilis</em> which was the first report.</p>


2019 ◽  
Vol 64 (6) ◽  
pp. 360-367
Author(s):  
I. S. Kosilova ◽  
L. V. Domotenko ◽  
N. K. Fursova ◽  
S. V. Dentovskaya ◽  
M. G. Ershova ◽  
...  

The results of the comparative tests of the «Agar Muller-Hinton II - Obolensk» nutrient medium developed in SRCAMB, Obolensk, and the control nutrient medium imported «Mueller Hinton II Agar» are presented in the study. The susceptibility of bacterial clinical strains to antimicrobial agents (AMP) was determined by the disc diffusion method and the method of gradient diffusion (E-test). The carbapenemase activity of the strains carrying the carbapenemase genes was determined by CIM-test. Total 173 characterized bacterial strains of species Klebsiella pneumoniae, Pseudomonas aeruginosa, Acinetobacter baumannii, Proteus mirabilis, Serratia marcescens, Enterobacter aerogenes, Escherichia coli; Photorhabdus spp., Staphylococcus aureus, Enterococcus spp. were used in the study, including producers of OXA- and NDM-types carbapenemases for gram negative bacteria. A high degree of coincidence of the results obtained on both nutrient media was shown. The consistency index of the strain sensitivity categories to AMPs (S, I, and R) was 98.2% for the disc diffusion method, and 94.4-100% - for E-test and CIM-test methods. Thus, within the framework of the Import Substitution Program, the domestic nutrient medium «MHA II-Obolensk» has been successfully developed. The nutrient medium meets the requirements of GOST R ISO 20776-2-2010 «Clinical laboratory testing and in vitro diagnostic test systems - Susceptibility testing of infectious agents and evaluation of performance of antimicrobial susceptibility test devices».


2007 ◽  
Vol 4 (s1) ◽  
pp. 17-20 ◽  
Author(s):  
Nenad Vukovic ◽  
Tanja Milosevic ◽  
Slobodan Sukdolak ◽  
Slavica Solujic

This study was designed to examine the chemical composition of essential oil and thein vitroantimicrobial activities of essential oil and methanol extract ofTeucrium montanum. The inhibitory effects of essential oil and methanol extracts ofT. montanumwere tested against 13 bacterial and three fungal species by using disc-diffusion method. GC/MS analyses revealed that essential oil contains mainly δ-cadinene (17.19%), β-selinene (8.16%) α-calacorene (4.97%), 1,6-dimethyl-4-(1-methylethyl)-naphthalene (4.91%), caryophyllene (4.35%), copaene (4.23%), torreyol (3.91%), 4-terpineol (3.90%), cadina-1,4-diene (3.39%), β-sesquiphellandrene (3.34%), τ-cadinol (3.12%) and γ-curcumene (3.18%). The essential oil has antibacterial as well as antifungal effect.


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