Search of Compounds with Antibacterial and Antifungal Activities Among New Derivatives of 3-benzylxanthine

Antimicrobial therapy is a significant element of modern medical and pharmaceutical practice. To create more effective medicines the researches are carried out among different classes of organic substances. One of the key strategies in this field is combination of several pharmacophores in a single molecule. In this aspect, the authors´ attention was attracted derivatives xantina, with a wide range of paid activity, and the large variability of the possibility of chemical modification. Objects of the study were derivatives of 3-benzyl-8-methylxanthinyl-7-acetic acid, synthesized by authors´ group previously. Antibacterial properties of these compounds were studied on Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa and antifungal activity on Candida albicans. It was found that the most active against Staphylococcus aureus compound was substance A-18, which according to this indicator significantly exceeded the Ampicillin. Compounds A-4, A-9, A-ll, A-13, A-19 by antistaphylococcal activity are not inferior to the Am-picillin. Ylidenhydrazide A-16 and S-substituted triazolylmethylxanthines A-22 and A-23 - surpassed it. It was also found that hydra-zide A-3, ylidenhydrazides A-6, A-ll - A-14 and A-17 showed fungistatic properties comparable to the Nystatin.

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Synthesis, characterization and biological activities of 1,3,4-oxadiazole derivatives of nalidixic acid and their copper complexes

10.31221/osf.io/g7mx8 ◽

2019 ◽

Author(s):

Chem Int

Keyword(s):

Nalidixic Acid ◽

Copper Complexes ◽

Biological Activities ◽

Bidentate Coordination ◽

Antibacterial And Antifungal Activities ◽

Elemental Analyses ◽

Oxadiazole Derivatives ◽

Antibacterial And Antifungal ◽

Derivatives Of ◽

Substituted 1

A series of novel 1, 3, 4-oxadiazole analogues was synthesized from cyclization of hydrazones of substituted 1-ethyl-1,4-dihydro-7-methyl-4-oxo-1,8-naphthyridine-3-carbohydrazides were prepared from nalidixic acid. The structures of synthesized oxadiazole derivatives and their copper complexes were elucidated on the basis of FTIR, elemental analyses, 1H-NMR and atomic absorption spectral analysis. It was observed from spectral data that metal ligand ratio was 1:1 in all copper complexes and they were bidentate, coordination was found to be done through oxygen of 4-oxo group and nitrogen of oxadiazole ring. The synthesized compounds were further evaluated with biological activities and compared with parent hydrazones. Copper complexes possess antibacterial and antifungal activities better than the oxadiazoles while they have better antioxidant activity then copper complexes. Parent hydrazones were better in all biological activities than synthesized oxadiazoles.

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Substituted 4-Formyl-2H-chromen-2-ones: Their Reaction with N-(2,3,4,6-Tetra-Oacetyl- β-D-galactopyranosyl)thiosemicarbazide, Antibacterial and Antifungal Activity of Their Thiosemicarbazone Products

Current Organic Chemistry ◽

10.2174/1385272824999200812132256 ◽

2020 ◽

Vol 24 (19) ◽

pp. 2272-2282

Author(s):

Vu Ngoc Toan ◽

Nguyen Minh Tri ◽

Nguyen Dinh Thanh

Keyword(s):

Escherichia Coli ◽

Staphylococcus Aureus ◽

Candida Albicans ◽

Selenium Dioxide ◽

Antibacterial And Antifungal Activity ◽

E Coli ◽

Antibacterial And Antifungal Activities ◽

Alkyl Ethers ◽

Antibacterial And Antifungal

Several 6- and 7-alkoxy-2-oxo-2H-chromene-4-carbaldehydes were prepared from corresponding alkyl ethers of 6- and 7-hydroxy-4-methyl-2-oxo-2H-chromen-2-ones by oxidation using selenium dioxide. 6- and 7-Alkoxy-4-methyl-2H-chromenes were obtained with yields of 57-85%. Corresponding 4-carbaldehyde derivatives were prepared with yields of 41-67%. Thiosemicarbazones of these aldehydes with D-galactose moiety were synthesized by reaction of these aldehydes with N-(2,3,4,6-tetra-O-acetyl-β-Dgalactopyranosyl) thiosemicarbazide with yields of 62-74%. These thiosemicarbazones were screened for their antibacterial and antifungal activities in vitro against bacteria, such as Staphylococcus aureus, Escherichia coli, and fungi, such as Aspergillus niger, Candida albicans. Several compounds exhibited strong inhibitory activity with MIC values of 0.78- 1.56 μM, including 8a (against S. aureus, E. coli, and C. albicans), 8d (against E. coli and A. niger), 9a (against S. aureus), and 9c (against S. aureus and C. albicans).

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Synthesis of the Bacteriostatic Poly(L-Lactide) by Using Zinc (II)[(acac)(L)H2O] (L = Aminoacid-Based Chelate Ligands) as an Effective ROP Initiator

International Journal of Molecular Sciences ◽

10.3390/ijms22136950 ◽

2021 ◽

Vol 22 (13) ◽

pp. 6950

Author(s):

Renata Barczyńska-Felusiak ◽

Małgorzata Pastusiak ◽

Piotr Rychter ◽

Bożena Kaczmarczyk ◽

Michał Sobota ◽

...

Keyword(s):

Schiff Bases ◽

Antibacterial Properties ◽

Antimicrobial Effect ◽

Zinc Complexes ◽

Antibacterial And Antifungal Activities ◽

Aspergillus Brasiliensis ◽

Acetylacetonate Complex ◽

Distorted Trigonal Bipyramid ◽

Composition Structure ◽

Antibacterial And Antifungal

The paper presents a synthesis of poly(l-lactide) with bacteriostatic properties. This polymer was obtained by ring-opening polymerization of the lactide initiated by selected low-toxic zinc complexes, Zn[(acac)(L)H2O], where L represents N-(pyridin-4-ylmethylene) tryptophan or N-(2-pyridin-4-ylethylidene) phenylalanine. These complexes were obtained by reaction of Zn[(acac)2 H2O] and Schiff bases, , the products of the condensation of amino acids and 4-pyridinecarboxaldehyde. The composition, structure, and geometry of the synthesized complexes were determined by NMR and FTIR spectroscopy, elemental analysis, and molecular modeling. Both complexes showed the geometry of a distorted trigonal bipyramid. The antibacterial and antifungal activities of both complexes were found to be much stronger than those of the primary Schiff bases. The present study showed a higher efficiency of polymerization when initiated by the obtained zinc complexes than when initiated by the zinc(II) acetylacetonate complex. The synthesized polylactide showed antibacterial properties, especially the product obtained by polymerization initiated by a zinc(II) complex with a ligand based on l-phenylalanine. The polylactide showed a particularly strong antimicrobial effect against Pseudomonas aeruginosa, Staphylococcus aureus, and Aspergillus brasiliensis. At the same time, this polymer does not exhibit fibroblast cytotoxicity.

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Convenient one pot synthesis of some novel derivatives of thiazolo[2,3-b]dihydropyrimidinone possessing 4-methylthiophenyl moiety and evaluation of their antibacterial and antifungal activities

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2006.09.003 ◽

2007 ◽

Vol 42 (3) ◽

pp. 380-385 ◽

Cited By ~ 122

Author(s):

Mithun Ashok ◽

Bantwal Shivarama Holla ◽

Nalilu Suchetha Kumari

Keyword(s):

One Pot ◽

Antifungal Activities ◽

One Pot Synthesis ◽

Antibacterial And Antifungal Activities ◽

Antibacterial And Antifungal ◽

Derivatives Of

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Antioxidant and Antimicrobial Activities of the Fresh aerial parts of Ammi visnaga L. from Algeria

South Asian Journal of Experimental Biology ◽

10.38150/sajeb.6(2).p70-76 ◽

2016 ◽

Vol 6 (2) ◽

pp. 70-76

Author(s):

Soumia Keddari ◽

Narimen Benaoum ◽

Yasmina Mokhtaria Boufadi ◽

Mansouria Belhocine ◽

Ali Riazi

Keyword(s):

Staphylococcus Aureus ◽

Antimicrobial Activity ◽

Phenolic Compounds ◽

Biological Activities ◽

Antibacterial Properties ◽

Ethanolic Extract ◽

Diffusion Method ◽

E Coli ◽

Ammi Visnaga ◽

Wide Range

Medicinal plants have been used for countries as cures for human diseases because they contain components of therapeutic value. Among these medi-cinal plants, Ammi visnage which have an immense reservoir of potential compounds attributed to the secondary metabolites which have the advan-tage of being of great diversity of chemical structure and have a very wide range of biological activities. The objectives of the present work were to stu-dy the antioxidant and antimicrobial activity of phenolic compounds ex-tracted from A. visnaga L. Its extraction is performed by two methods, etha-nol extraction and water extraction. The results showed that A. visnaga L.. ethanolic extract contains a mixture of phytochemical classes as polyphenol, flavonoids and revealed that this plant has high antioxidant activity (IC50 0.069 mg/ml). Regarding the antimicrobial activity results expressed by the diameter of the inhibition zones by diffusion method AWDT, the most signifi-cant inhibition was observed against to Staphylococcus aureus (12 mm) to the ethanol extract at concentration of 100mg / ml. Thus the aqueous ex-tract had a significant inhibitory activity against on the strains Staphylococ-cus aureus (8 mm), E. coli ATCC 10536 (8 mm) to a concentration of 100 mg / ml. The results for the antibacterial properties have shown that Gram-positive bacteria (Staphylococcus aureus, Listeria monocytogenes and M. luteus.) were more sensitive than gram-negative (Pseudomonas aeruginosa, E. coli ATCC 10536) against from the action of phenolic compounds of the Ammi visnaga ethanolic extract.

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Studies on Antibacterial and Antifungal Activities of Some Derivatives of Tributyltin (IV) of Salicylic Acid

10.9734/bpi/nvst/v2/3899f ◽

2021 ◽

pp. 128-132

Author(s):

Pankaj Mittal

Keyword(s):

Salicylic Acid ◽

Antifungal Activities ◽

Antibacterial And Antifungal Activities ◽

Antibacterial And Antifungal ◽

Derivatives Of

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Synthesis and investigation of 3,5-bis-linear and macrocyclic tripeptidopyridine candidates by using l-valine, N,N′-(3,5-pyridinediyldicarbonyl)bis-dimethyl ester as synthon

Zeitschrift für Naturforschung B ◽

10.1515/znb-2019-0006 ◽

2019 ◽

Vol 74 (6) ◽

pp. 473-478 ◽

Cited By ~ 2

Author(s):

Abd El-Galil E. Amr ◽

Ahmed M. Naglah ◽

Nermien M. Sabry ◽

Alhussein A. Ibrahim ◽

Elsayed A. Elsayed ◽

...

Keyword(s):

Staphylococcus Aureus ◽

Candida Albicans ◽

Organic Molecules ◽

Biological Activities ◽

Dimethyl Ester ◽

Antimicrobial Activities ◽

Current Work ◽

Antifungal Activities ◽

Antibacterial And Antifungal Activities ◽

Antibacterial And Antifungal

AbstractInterest in the synthesis of heterocyclic organic molecules with peptide moieties has gained attention due to their potential biological activities. The current work aimed at synthesizing new macrocyclic tripeptide imides and evaluating their possible antimicrobial activities. A series of 11 derivatives were prepared from dimethyl 3,5-pyridinevalinyl ester either by NaOH or NH2NH2 treatment, followed by cyclization and further reaction with NaOH or NH2NH2. The majority of synthesized derivatives showed promising antibacterial and antifungal activities in comparison to standard known antibiotics. Compounds 5a and 7b showed the most potential antibacterial against Staphylococcus aureus and antifungal activities against Candida albicans, respectively.

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Synthesis of New Oxindoles and Determination of Their Antibacterial Properties

Heteroatom Chemistry ◽

10.1155/2020/8021920 ◽

2020 ◽

Vol 2020 ◽

pp. 1-9

Author(s):

Pablo E. Romo ◽

Braulio Insuasty ◽

Rodrigo Abonia ◽

María del Pilar Crespo ◽

Jairo Quiroga

Keyword(s):

Staphylococcus Aureus ◽

Antibacterial Activity ◽

Neisseria Gonorrhoeae ◽

Room Temperature ◽

Antibacterial Properties ◽

Analytical Techniques ◽

Toluenesulfonic Acid ◽

Antistaphylococcal Activity ◽

New Compounds

A versatile method for the synthesis of new oxindoles was developed by the reaction between substituted isatins and 5-aminopyrazoles. The reaction was carried out at room temperature in ethanol using p-toluenesulfonic acid as the catalyst. The products were obtained with acceptable to excellent yields (44–96%). Structures of the new compounds were unambiguously established by spectroscopic and analytical techniques. The antibacterial activity was determined by microdilution assays. Compounds 3b, 3e, and 3g showed antistaphylococcal activity, particularly compound 3e displayed a potent activity against the vancomycin intermediate Staphylococcus aureus (VISA). Compounds 3i, 3j, and 3o inhibited Neisseria gonorrhoeae growth.

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(–)-Agelasidine A from Agelas clathrodes

Zeitschrift für Naturforschung C ◽

10.1515/znc-2006-7-802 ◽

2006 ◽

Vol 61 (7-8) ◽

pp. 472-476 ◽

Cited By ~ 9

Author(s):

Maria Augusta Medeiros ◽

Ana Lourenço ◽

Maria Regina Tavares ◽

Maria João Marcelo Curto ◽

Sónia Savluchinske Feio ◽

...

Keyword(s):

Staphylococcus Aureus ◽

Marine Sponge ◽

Methanol Extract ◽

Spectroscopic Methods ◽

Antifungal Activities ◽

Antibacterial And Antifungal Activities ◽

Bacteriostatic Agent ◽

Antibacterial And Antifungal ◽

First Time

(-)-Agelasidine A was identified from the methanol extract of the marine sponge Agelas clathrodes for the first time together with zooanemonin, 1-carboxymethylnicotinic acid, hymenidin, mukanadins A and C, monobromodispacamide, agelasidine D, 2-amide-4-bromopyrrole, O-methyltryptophan and an agelasines mixture. The structures were characterized by spectroscopic methods. (-)-Agelasidine A was tested for antibacterial and antifungal activities and shown to act as a bacteriostatic agent as it inhibited the growth of Staphylococcus aureus and partially the growth of other bacteria.

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