scholarly journals Synthesis and Characterization of Some NH-Analogues of Ciprofloxacin on Antibacterial, Antifungal, and Cytotoxic Activities

2020 ◽  
Vol 12 (3) ◽  
pp. 349-362
Author(s):  
M. G. Rabbani ◽  
M. R. Islam
Keyword(s):  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Cytotoxic Activities ◽  
Bacterial Strains ◽  
Mass Spectral Data ◽  
Disc Diffusion Method ◽  
Mass Spectral ◽  
Brine Shrimp Lethality Assay ◽  
Ft Ir

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.

Synthesis and Characterization of Some Mannich Base Analogues of Ciprofloxacin: Antibacterial, Antifungal, and Cytotoxic Activities

2021 ◽  
Vol 13 (2) ◽  
pp. 545-559
Author(s):  
M. G. Rabbani ◽  
M. R. Islam
Keyword(s):  
Mannich Base ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Cytotoxic Activities ◽  
Therapeutic Assessment ◽  
Bacterial Strains ◽  
Brine Shrimp Lethality Assay ◽  
Ft Ir ◽  
The Mannich Reaction

The present work contains synthesis of six Mannich base analogues of ciprofloxacin 2-7 those have been prepared by the Mannich reaction to investigate some therapeutic assessment. The structure of the analogues has been established by FT-IR, 1H NMR, 13C NMR, mass spectroscopy, and elemental analysis techniques. The derivatives were screened for their antimicrobial activities by the disc diffusion method. The antimicrobial activity of the analogues compared with the parent was evaluated against three Gram-positive, eight Gram-negative bacterial strains, and three different fungal strains. The synthesized compounds showed diverse antimicrobial profiles among which derivatives 2, 3 & 6 possessed enhanced activity in contrast to the ciprofloxacin. Additionally, unlike ciprofloxacin, most of the derivatives were found to demonstrate antifungal activity against Candida albicans.  Cytotoxicity was also made against brine shrimp lethality assay. Interestingly, most of the derivatives revealed enhanced cytotoxic activity than that of ciprofloxacin.

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
Keyword(s):  
Transition Metal ◽  
Transition Metal Complexes ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Molar Conductivity ◽  
Diffusion Method ◽  
Disc Diffusion ◽  
Bacterial Strains ◽  
Disc Diffusion Method ◽  
Brine Shrimp Lethality Assay

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.

scholarly journals Synthesis and Antimicrobial Activity ofSome New 2-Substituted Benzothiazole Derivatives

2009 ◽  
Vol 6 (3) ◽  
pp. 775-779 ◽  
Author(s):  
B. Rajeeva ◽  
N. Srinivasulu ◽  
S. M. Shantakumar
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Data ◽  
Diffusion Method ◽  
Disc Diffusion ◽  
Phosphoryl Chloride ◽  
Mass Spectral Data ◽  
Disc Diffusion Method ◽  
Mass Spectral ◽  
Benzothiazole Derivatives ◽  
H Nmr

Some new 2-(5-substituted-1,3,4-oxadiazole-2-yl)-1,3- benzothiazole(3a-j)were synthesized by refluxing benzothiazolyl carboxyhydrazide with different aryl acids in phosphoryl chloride. Structures of the synthesized compounds were established on the basis of1H NMR and Mass spectral data. The anti microbial activity of the synthesized compounds was evaluated by disc diffusion method.

scholarly journals Synthesis and Characterization of ZnO-Nanocomposites by Utilizing Aloe Vera Leaf Gel and Extract of Terminalia arjuna Nuts and Exploring Their Antibacterial Potency

2021 ◽  
Vol 2021 ◽  
pp. 1-7
Author(s):  
Amara Dar ◽  
Rabia Rehman ◽  
Warda Zaheer ◽  
Umer Shafique ◽  
Jamil Anwar
Keyword(s):  
Aloe Vera ◽  
Diffusion Method ◽  
Synthesis And Characterization ◽  
Terminalia Arjuna ◽  
Disc Diffusion ◽  
Bacterial Strains ◽  
Disc Diffusion Method ◽  
Environment Friendly ◽  
E Coli

Nanotechnology has found vast applications in everyday life. Use of plant extract in the synthesis of nanocomposites produces relatively less toxic and environment-friendly materials. The present study deals with the synthesis of zinc oxide nanocomposite using gel from leaves of Aloe vera (black Aloe vera (BAV) and white Aloe vera (WAV)) and extract from powder of nuts of Terminalia arjuna. Synthesized nanocomposites were then characterized by using SEM, FTIR, and UV-Vis techniques. Disc diffusion method was opted to inquire the antimicrobial ability of nanocomposites against different bacterial strains such as Escherichia coli (−) and Burkholderia stabilis (+). ZnO-BAV possessed good antimicrobial potential against both selected strains as proved from zone of inhibitions. However, ZnO-WAV and ZnO-N showed potential against E. coli and no response for B. stabilis.

scholarly journals Synthesis and Characterization of Some Novel Coumarin Based 2-Pyridone Heterocycles with their Broad Spectrum Antimicrobial Potency

2016 ◽  
Vol 66 ◽  
pp. 1-12 ◽  
Author(s):  
Nisheeth C. Desai ◽  
Tushar J. Karkar
Keyword(s):  
Antimicrobial Activity ◽  
Synthesis And Characterization ◽  
Bacterial Strains ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
H Nmr ◽  
Bacteria And Fungi ◽  
Broth Dilution ◽  
C Nmr

The synthesis of a novel series of 6-((arylidene) amino)-2-oxo-1-((1-(2-oxo-2H-chromen-3-yl) ethylidene) amino)-4-phenyl-1,2-dihydropyridine-3,5-dicarbonitriles 4a-o were synthesized and structures of compounds have been elucidated by IR,1H NMR,13C NMR and mass spectral data. Antimicrobial activity was measured against certain strains of bacteria and fungi by serial broth dilution. Evaluation of antimicrobial activity shown that the compounds (4g, 4j, 4k and 4o) were found to be most active against selected bacterial strains and compounds (4d, 4m and 4n) were found to be most active against selected fungal strains.

scholarly journals Synthesis and Antimicrobial Activity of Quinazolinone Conjugated Peptides

2010 ◽  
Vol 7 (2) ◽  
pp. 449-456 ◽  
Author(s):  
G. P. Suresha ◽  
K. C. Prakasha ◽  
Wethroe Kapfo ◽  
D. Channe Gowda
Keyword(s):  
Antimicrobial Activity ◽  
Chain Length ◽  
Alkyl Chain ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Antimicrobial Compounds ◽  
Bacterial Strains ◽  
Butanoic Acid ◽  
Disc Diffusion Method ◽  
Structure Activity

Antimicrobial compounds were synthesized by coupling 4-(4-oxo-3,4-dihydroquinazolin-2-yl) butanoic acid with VP, GVP, VGVP and GVGVP peptides. Antimicrobial activities of the synthesized compounds were performed against various bacterial strains by disc diffusion method. The structure activity relationship was evaluated with respect to hydrophobicity, polarity, chain length of peptides and alkyl chain length of quinazolinone. Correlations of analogs with respect to their antimicrobial activity in comparison with conventional drugs and probable mechanism for the activity were discussed.

scholarly journals Synthesis and antimicrobial activities of novel n-substituted 8-(1-alkyl/alkylsulphonyl/alkoxycarbonyl-benzimidazol-2-ylmethoxy)-5-chloroquinolines

2011 ◽  
Vol 76 (9) ◽  
pp. 1199-1206 ◽  
Author(s):  
Raju Chaudhari ◽  
Sahebrao Rindhe
Keyword(s):  
Staphylococcus Aureus ◽  
Antibacterial Activity ◽  
Nitrogen Heterocycles ◽  
Antimicrobial Activities ◽  
Mass Spectral Data ◽  
Antifungal Activities ◽  
Mass Spectral ◽  
Electrophilic Reagents ◽  
Almost All ◽  
And Staphylococcus Aureus

Herein the synthesis of a series of novel 8-(1- alkyl/alkylsulphonyl/alkoxycarbonyl-benzimidazol-2-ylmethoxy)-5- chloroquinoline derivatives is reported. These derivatives were prepared by the condensation of o-phenylenediamine with [(5-chloroquinolin-8- yl)oxy]acetic acid, followed by substitution at nitrogen with different electrophilic reagents in presence of an appropriate base to give a series of nitrogen heterocycles containing the benzimidazole and quinoline nuclei. The structures of the compounds were confirmed based on 1H-NMR, 13CNMR, IR and mass spectral data. Almost all the compounds exhibited promising antibacterial activity against Salmonella typhimurium and Staphylococcus aureus. Some of the compounds showed good antifungal activities against Aspergillus niger but the antifungal activities against Candida albicans were disappointing.

scholarly journals The PHYTOCHEMICALS, ANTIOXIDANT AND ANTIMICROBIAL PROPERTIES OF Senna alata AND Senna tora LEAF EXTRACTS AGAINST BACTERIAL STRAINS CAUSING SKIN INFECTIONS

2019 ◽  
Vol 2 (1) ◽  
pp. 19
Author(s):  
Murni Halim
Keyword(s):  
Leaf Extract ◽  
Antimicrobial Properties ◽  
Inhibition Zone ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Leaf Extracts ◽  
Natural Drugs ◽  
Senna Alata

A study was carried out to screen for phytochemical constituents and assess the antioxidant and antimicrobial activities of Senna alata and Senna tora leaf extracts. The leaves were first dried at room temperature and 50°C in an oven prior to solvent extraction using ethanol and methanol. The in-vitro qualitative assays showed that both S. alata and S. tora leaf extracts contained bioactive and secondary metabolites components such as tannins, steroids, saponin, terpenoids, glycosides, flavonoids and phenols. The antioxidant activity and capacity test were carried out by conducting free radical of 2,2-diphenyl-1-picrylhydrazyl (DPPH) scavenging activity and Ferric reduction antioxidant plasma (FRAP) assays. Both assays showed S. tora leaf extract has higher antioxidant capacity than S. alata leaf extract. The efficacy of these leaf extracts were tested against skin pathogens through agar well diffusion method. S. alata extract showed an inhibition zone (1.15 – 1.59 mm) against Pseudomonas aeruginosa while S. tora extracts exhibited a strong antimicrobial activity against S. epidermidis (inhibition zone of 12 – 16.94 mm) followed by P. aeruginosa (inhibition zone of 1 – 1.59 mm). Nonetheless, no inhibition zone was observed for S. aureus by both leaf extracts. The phytochemicals and antioxidant constituents as well as inhibitory potential on skin pathogens possessed by S. alata and S. tora leave highlighted their potential utilization in the development of natural drugs or cosmetics to treat skin related diseases or infections.

scholarly journals Synthesis and Characterization of Cobalt(III) and Copper(II) Complexes of 2-((E)-(6-Fluorobenzo[d]thiazol-2-ylimino) methyl)-4-chlorophenol: DNA Binding and Nuclease Studies—SOD and Antimicrobial Activities

2018 ◽  
Vol 2018 ◽  
pp. 1-15 ◽  
Author(s):  
K. Savithri ◽  
B. C. Vasantha Kumar ◽  
H. K. Vivek ◽  
H. D. Revanasiddappa
Keyword(s):  
Metal Complexes ◽  
Antimicrobial Activities ◽  
Spectroscopic Studies ◽  
Docking Studies ◽  
Bacterial Strains ◽  
Spectral Techniques ◽  
Light Reduction ◽  
Drug Candidates ◽  
Ft Ir

A bidentate (N- and O-) imine-based ligand (L1) and its metal complexes of types [CuII(L1)2] (C1), [CuII(L1)(Phen)] (C2), [CoIII(L1)2] (C3), and [CoIII(L1)(Phen)] (C4) (L1 = 2-((E)-(6-fluorobenzo[d]thiazol-2-ylimino)methyl)-4-chlorophenol and phen = 1,10-phenanthroline) were synthesized as potential chemotherapeutic drug candidates. The prepared complexes were structurally characterized by spectral techniques (NMR, FT-IR, LC-MS, EPR, and electronic absorption), thermogravimetric analysis (TGA/DTA), magnetic moment, and CHNO elemental analysis. Spectroscopic studies suggested the distorted octahedral structure for all complexes. In vitro bioassay studies include binding and nuclease activities of the ligand and its complexes with target calf thymus- (CT-) DNA were carried out by employing UV-Vis, fluorescence spectroscopy, viscosity, and gel electrophoresis techniques. The extent of binding propensity was determined quantitatively by Kb and Ksv values which revealed a higher binding affinity for C2 and C4 as compared to C1 and C3. In addition, the scavenging superoxide anion free radical (O∙-2) activity of metal complexes was determined by nitroblue tetrazolium (NBT) light reduction assay. Molecular docking studies with DNA and SOD enzyme were also carried out on these compounds. The antimicrobial study has shown that all the compounds are potential antibacterial agents against Gram-negative bacterial strains and better antifungal agents with respect to standard drugs used.

scholarly journals Synthesis, Biological Assessment, and Structure Activity Relationship Studies of New Flavanones Embodying Chromene Moieties

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 544 ◽  
Author(s):  
Eman Assirey ◽  
Azhaar Alsaggaf ◽  
Arshi Naqvi ◽  
Ziad Moussa ◽  
Rawda M. Okasha ◽  
...  
Keyword(s):  
In Silico ◽  
Biological Assessment ◽  
Diffusion Method ◽  
Breast Adenocarcinoma ◽  
Cytotoxic Activities ◽  
Human Pathogens ◽  
Bacterial Strains ◽  
Human Carcinoma ◽  
In Silico Studies

Novel flavanones that incorporate chromene motifs are synthesized via a one-step multicomponent reaction. The structures of the new chromenes are elucidated by using IR, 1H-NMR, 13C-NMR, 1H-1H COSY, HSQC, HMBC, and elemental analysis. The new compounds are screened for their in vitro antimicrobial and cytotoxic activities. The antimicrobial properties are investigated and established against seven human pathogens, employing the agar well diffusion method and the minimum inhibitory concentrations. A majority of the assessed derivatives are found to exhibit significant antimicrobial activities against most bacterial strains, in comparison to standard reference drugs. Moreover, their cytotoxicity is appraised against four different human carcinoma cell lines: human colon carcinoma (HCT-116), human hepatocellular carcinoma (HepG-2), human breast adenocarcinoma (MCF-7), and adenocarcinoma human alveolar basal epithelial cell (A-549). All the desired compounds are subjected to in-silico studies, forecasting their drug likeness, bioactivity, and the absorption, distribution, metabolism, and excretion (ADME) properties prior to their synthetic assembly. The in-silico molecular docking evaluation of all the targeted derivatives is undertaken on gyrase B and the cyclin-dependent kinase. The in-silico predicted outcomes were endorsed by the in vitro studies.

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