scholarly journals Axially Ligated Zirconium(IV) Tetraphenylporphyrin: Synthesis, Characterization, and Biological Activity

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Gauri D. Bajju ◽  
Sunil Kumar Anand ◽  
Gita Devi

A series of 5,10,15,20-tetraphenylporphinatozirconium(IV) acetylacetonatophenolates containing different phenols as axial ligands [Zr(TPP)(Y)(X)] (TPP = 5,10.15,20-tetraphenyl-21H, 23H-porphine; Y = acac; X = different phenolates) have been synthesized and characterized by various spectrochemical studies. The complexes were also screened for antimicrobial activities. Antifungal activity of some adducts has been carried out against the fungal strain Sclerotium rolfsii. Most of the complexes have shown good antibacterial activity.

2019 ◽  
Vol 70 (10) ◽  
pp. 3603-3610
Author(s):  
Madalina Mihalache ◽  
Cornelia Guran ◽  
Aurelia Meghea ◽  
Vasile Bercu ◽  
Ludmila Motelica ◽  
...  

The three copper complexes having a-ketoglutaric acid (H2A) and 1- (o-tolyl) biguanide (TB) ligands have been synthesized and characterized. The proposed formulas for these complexes are: [Cu(TB)(HA)]Cl (C1), [Cu(TB)(HA)CH3COO]�H2O (C2) and [Cu(TB)(HA)](NO3) (C3) where HA represents deprotonated H2A. The complexes obtained were tested for antibacterial activity against Staphylococcus aureus ATCC 25923 and Pseudomonas aeruginosa ATCC 27853, antifungal activity on Candida albicans ATCC 10231 and antitumor activity on HeLa tumor cells. Due to the antitumor, antifungal, antimicrobial activity and inhibition of inert substrate adhesion, complexes synthesized could be used for potential therapeutic applications.


2020 ◽  
Vol 15 (6) ◽  
pp. 665-679
Author(s):  
Alok K. Srivastava ◽  
Lokesh K. Pandey

Background: [1, 3, 4]oxadiazolenone core containing chalcones and nucleosides were synthesized by Claisen-Schmidt condensation of a variety of benzaldehyde derivatives, obtained from oxidation of substituted 5-(3/6 substituted-4-Methylphenyl)-1, 3, 4-oxadiazole-2(3H)-one and various substituted acetophenone. The resultant chalcones were coupled with penta-O-acetylglucopyranose followed by deacetylation to get [1, 3, 4] oxadiazolenone core containing chalcones and nucleosides. Various analytical techniques viz IR, NMR, LC-MS and elemental analysis were used to confirm the structure of the synthesised compounds.The compounds were targeted against Bacillus subtilis, Staphylococcus aureus and Escherichia coli for antibacterial activity and Aspergillus flavus, Aspergillus niger and Fusarium oxysporum for antifungal activity. Methods: A mixture of Acid hydrazides (3.0 mmol) and N, Nʹ- carbonyl diimidazole (3.3 mmol) in 15 mL of dioxane was refluxed to afford substituted [1, 3, 4]-oxadiazole-2(3H)-one. The resulted [1, 3, 4]- oxadiazole-2(3H)-one (1.42 mmol) was oxidized with Chromyl chloride (1.5 mL) in 20 mL of carbon tetra chloride and condensed with acetophenones (1.42 mmol) to get chalcones 4. The equimolar ratio of obtained chalcones 4 and β -D-1,2,3,4,6- penta-O-acetylglucopyranose in presence of iodine was refluxed to get nucleosides 5. The [1, 3, 4] oxadiazolenone core containing chalcones 4 and nucleosides 5 were tested to determined minimum inhibitory concentration (MIC) value with the experimental procedure of Benson using disc-diffusion method. All compounds were tested at concentration of 5 mg/mL, 2.5 mg/mL, 1.25 mg/mL, 0.62 mg/mL, 0.31 mg/mL and 0.15 mg/mL for antifungal activity against three strains of pathogenic fungi Aspergillus flavus (A. flavus), Aspergillus niger (A. niger) and Fusarium oxysporum (F. oxysporum) and for antibacterial activity against Gram-negative bacterium: Escherichia coli (E. coli), and two Gram-positive bacteria: Staphylococcus aureus (S. aureus) and Bacillus subtilis(B. subtilis). Result: The chalcones 4 and nucleosides 5 were screened for antibacterial activity against E. coli, S. aureus and B. subtilis whereas antifungal activity against A. flavus, A. niger and F. oxysporum. Compounds 4a-t showed good antibacterial activity whereas compounds 5a-t containing glucose moiety showed better activity against fungi. The glucose moiety of compounds 5 helps to enter into the cell wall of fungi and control the cell growth. Conclusion: Chalcones 4 and nucleosides 5 incorporating [1, 3, 4] oxadiazolenone core were synthesized and characterized by various spectral techniques and elemental analysis. These compounds were evaluated for their antifungal activity against three fungi; viz. A. flavus, A. niger and F. oxysporum. In addition to this, synthesized compounds were evaluated for their antibacterial activity against gram negative bacteria E. Coli and gram positive bacteria S. aureus, B. subtilis. Compounds 4a-t showed good antibacterial activity whereas 5a-t showed better activity against fungi.


2021 ◽  
Vol 3 (1) ◽  
pp. 1-5
Author(s):  
Poonam Sethi ◽  
Nandhagopal Karmegam

ABSTRACT Artabotrys odoratissimus R.Br.  (Annonaceae) a medium sizes shrub with hooks, sweet smelling flowers and aggregate fruits, was tested for activity against gram negative bacteria. The fruit of the experimental plant was extracted with water, methanol and toluene: methanol (2:1 v/v). Artabotrys fruits showed good antibacterial activity and produced zone of inhibition of 32mm. The methanolic extract of the fruit showed maximum zone of inhibition at 300 ?g/ml against Pseudomonas fluorescens. The present study clearly indicates that A. odoratissimus had a profound antimicrobial   activity and it may be useful in the treatment of various infectious caused by bacteria. Keywords: Artabotrys, Gram Negative Bacteria, Pseudomonas, Zone Of Inhibition


2010 ◽  
Vol 7 (2) ◽  
pp. 545-550
Author(s):  
Kumar Sanjeev S. Lamani ◽  
Oblennavar Kortesh

A novel and efficient route have been designed for the synthesis of 4-(5-mercapto-1,3,4-thiadiazol-2-yl)-2-phenyl-5-[2-phenylvinyl]-2,4-dihydro-3H-1,2,4-triazol-3-one. All the synthesized compound were characterized by elemental analysis, IR,1H NMR,13C NMR and mass spectra. All the synthesized products were evaluated for their antibacterial activity againstB. SubtilisandE.Coliand antifungal activity againstA. nigerandC.Albicanrespectively. The results indicate that the present compounds may serve as better fungicides when compared to bactericides. The synthesized compounds have turned to be wonder by possessing antimicrobial properties.


2008 ◽  
Vol 5 (4) ◽  
pp. 963-968 ◽  
Author(s):  
Sabir Hussain ◽  
Jyoti Sharma ◽  
Mohd Amir

Various 4-amino-2-[4-(4-substituted phenyl)-5-sulfanyl-4H-1,2,4-triazol-3-yl] phenol (4a-c), 4-amino-2-{4-amino-5-[(4-substituted phenyl)amino]-4H-1,2,4-triazol-3-yl} phenol (5a-c) and 4-amino-2-{5-[(4-substituted phenyl)amino]-1,3,4-thiadiazole-2-yl} phenol (6a-g) were synthesized and evaluated for their antibacterial and antifungal activity. The compounds showed significant antibacterial activity againstS. aureus(gram-positive) andE.coli(gram-negative) bacteria and antifungal activity againstA. nigerfungi using cup plate technique


2019 ◽  
Vol 62 (4) ◽  
Author(s):  
Idhayadhulla Akbar ◽  
Anis Ahamed ◽  
Ibrahim A. Arif ◽  
Radhakrishnan Surendra Kumar ◽  
Keerthana Selva raj ◽  
...  

A series of novelpyridine-connected piperidine derivatives (2a-g) and pyridine-connected 2H-thiopyran derivatives (4a-g) were synthesized and screened for larvicidal, nematicidal, and antimicrobial activities. Compound 4e exhibited larvicidal activity against second instar larvae with an LD50 value of 0.8μg/mL. In addition, 4e exhibited high nematicidal activity, with an LD50 value of 3.2μg/mL.Compounds 2e (MIC: 4 μg/mL) and 2d (MIC: 4 μg/mL) exhibited high antibacterial activity against Klebsiella pneumoniae and Escherichia coli, respectively. Compounds 4b (MIC: 0.25 μg/mL) and 4f (MIC: 2 μg/mL) showed high antifungal activity against Candida albicans and Microsporum audouinii, respectively. Therefore, it can be suggested that compounds 2e, 2d, 4e, 4b, and 4f may be useful as lead molecules for the development of new classes ofdrugs with larvicidal,nematicidal,and antimicrobial activities.


2019 ◽  
Vol 70 (10) ◽  
pp. 3603-3610

The three copper complexes having a-ketoglutaric acid (H2A) and 1- (o-tolyl) biguanide (TB) ligands have been synthesized and characterized. The proposed formulas for these complexes are: Cl (C1), •H2O (C2) and (NO3) (C3) where HA represents deprotonated H2A. The complexes obtained were tested for antibacterial activity against Staphylococcus aureus ATCC 25923 and Pseudomonas aeruginosa ATCC 27853, antifungal activity on Candida albicans ATCC 10231 and antitumor activity on HeLa tumor cells. Due to the antitumor, antifungal, antimicrobial activity and inhibition of inert substrate adhesion, complexes synthesized could be used for potential therapeutic applications. Keywords: 1-(o-tolyl)biguanide, a-ketoglutaric acid, copper complexes, antibacterial activity, celule HeLa, antifungal activity


2021 ◽  
Vol 6 (3) ◽  
pp. 181-185
Author(s):  
S. Syed Shafi ◽  
R. Rajesh ◽  
S. Senthilkumar

In present work, ethyl 2-aminobenzo[d]thiazole-6-carboxylate was reacted to piperidine using copper(II) bromide to get ethyl 2-(piperidin-1-yl)benzo[d]thiazole-6-carboxylate. The reaction of ethyl 2-(piperidin- 1-yl)benzo[d]thiazole-6-carboxylate with NaOH produces 2-(piperidin-1-yl)benzo[d]thiazole-6- carboxylic acid. The inter-mediate 2-(piperidin-1-yl)benzo[d]thiazole-6-carboxylic acid have been isolated as stable compounds. The chemical structures of synthesized compounds were established based on the 1H & 13C NMR and IR spectral data. The mass of the novel compounds was established with the help of the LC-MS technique. The photoluminescence spectra explain the optical property of the compound. The biological studies of synthesized compounds show that the compound 5e possesses good antibacterial activity and compound 5d has good antifungal activity.


INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (08) ◽  
pp. 18-24
Author(s):  
Umakant ◽  
◽  
D. Sharma ◽  
D. Pathak ◽  
G. Sharma ◽  
...  

In the present work, some newer 3,5-substituted diphenyl isoxazole derivatives (compounds 1-10) were synthesised by reaction of hydroxylamine hydrochloride with various freshly synthesised 1-(substituted phenyl)-3-(substituted phenyl)prop-2en-1-one derivatives (compounds. 1A-10A) in the presence of pyridine and catalytic amount of sodium hydroxide. Compounds 2, 4, 5, 10 were found to possess good antibacterial activity and compounds 3 and 10 showed good antifungal activity when compared with standard drugs ciprofloxacin and fluconazole at the concentration 50 μg mL-1. These results suggest that the synthesized isoxazole derivatives exhibit promising activity and this work may pave the way for future development of promising compounds for this purpose.


2018 ◽  
Vol 16 (1) ◽  
pp. 93-100
Author(s):  
Hind Benouda ◽  
Btissam Bouchal ◽  
Allal Challioui ◽  
Abdelkader Oulmidi ◽  
Tarik Harit ◽  
...  

Background: A series of chalcones and flavones were synthesized from 2’-hydroxyacetophenone and substituted aromatic aldehydes via Simmons-Schmidt condensation followed by oxidative cyclization. Methods: Characterization of the obtained structures was established on the basis of their spectroscopic data. The synthesized compounds were screened for their antimicrobial activities against five bacterial strains (Citrobacter freundii, Staphylococcus aureus, Listeria monocytogenes, Salmonella braenderup, Escherichia coli.) and two fungal strains (Candida albicans, Candida krusei). Results: The in vitro bioassay results indicated that some target compounds displayed moderate (4d, 4e) to high (4a) antifungal activity against the pathogenic fungi C. albicans and C. krusei. Conclusion: For the antibacterial activity, only products 3d and 4d showed a weak antibacterial activity. These compounds can lead to the design of new drugs with specific antifungal activity.


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