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

2019 ◽  
Vol 74 (6) ◽  
pp. 473-478 ◽  
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.

scholarly journals Effect of Extraction Methods on Polyphenols, Flavonoids, Mineral Elements, and Biological Activities of Essential Oil and Extracts of Mentha pulegium L.

Molecules ◽  
2021 ◽  
Vol 27 (1) ◽  
pp. 11
Author(s):  
Mohammed Messaoudi ◽  
Abdelkrim Rebiai ◽  
Barbara Sawicka ◽  
Maria Atanassova ◽  
Hamza Ouakouak ◽  
...  
Keyword(s):  
Candida Albicans ◽  
Essential Oil ◽  
Biological Activities ◽  
Emission Spectrometry ◽  
Mentha Pulegium ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Pharmaceutical Industries ◽  
Anti Inflammatory ◽  
Antibacterial And Antifungal

Our study evaluated the in vitro antioxidant properties, antibacterial and antifungal activities, anti-inflammatory properties, and chemical composition of the essential oils (EOs), total phenol, and total flavonoid of wild Mentha pulegium L. This study also determined the mineral (nutritional and toxic) elements in the plant. The EOs were extracted using three techniques—hydro distillation (HD), steam distillation (SD), and microwave-assisted distillation (MAD)—and were analyzed using chromatography coupled with flame ionization (GC-FID) and gas chromatography attached with mass spectrometry detector (GC-MS). The antioxidant effects of the EOs were tested with 2,2-diphenyl-1-picrylhydrazyl (DPPH) and ABTS (2,2’-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid), while the antibacterial and antifungal activities of the EO and methanolic extract were tested using Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa, Escherichia coli, and Candida albicans. Twenty-six compounds were identified in the essential oil, representing 97.73% of the total oil, with 0.202% yield. The major components were pulegone (74.81%), menthone (13.01%) and piperitone (3.82%). Twenty-one elements, including macro- and micro-elements (Ba, Br, Ca, Cl, Co, Cr, Cs, Eu, Fe, K, Mg, Mn, Mo, Na, Rb, Sb, Sc, Sr, Th, U and Zn), were detected using neutron activation analysis (INAA) and inductively coupled plasma optical emission spectrometry (ICP-OES), with the concentration of mineral element close to the FAO recommendation. The results show that the EOs and extracts from Mentha pulegium L. had significant antimicrobial activities against the microorganisms, including five human pathogenic bacteria, one yeast (Candida albicans), and one phytopathogenic fungi. The in vivo anti-inflammatory activities of the leaf extracts were confirmed. The results indicate that the EOs and extracts from Mentha pulegium L. have promising applications in the pharmaceutical industries, clinical applications, and in medical research.

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

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).

Synthesis of a Series of Novel 2-Amino-5-Substituted 1,3,4-oxadiazole and 1,3,4-thiadiazole Derivatives as Potential Anticancer, Antifungal and Antibacterial Agents

2021 ◽  
Vol 17 ◽  
Author(s):  
Em Canh Pham ◽  
Tuyen Ngoc Truong ◽  
Nguyen Hanh Dong ◽  
Duy Duc Vo ◽  
Tuoi Thi Hong Do
Keyword(s):  
Cell Line ◽  
Biological Activities ◽  
Chemical Properties ◽  
Diffusion Method ◽  
Anticancer Activities ◽  
Molecular Docking Study ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Thiadiazole Derivatives ◽  
Antibacterial And Antifungal

Background: Many compounds containing a five-membered heterocyclic ring display exceptional chemical properties and versatile biological activities. Objective: The objective of the present study was the desire to prepare the 5-substituted 2-amino-1,3,4-oxadiazole and 2-amino-1,3,4-thiadiazole derivatives and evaluate their potential anticancer, antibacterial and antifungal activities. Methods: Twenty-seven derivatives were synthesized by iodine-mediated cyclization of semicarbazones or thiosemicarbazones obtained from condensation of semicarbazide or thiosemicarbazide and aldehydes. The structures were confirmed by 1H-NMR, 13C-NMR and MS spectra. The antibacterial and antifungal activities were evaluated by diffusion method and the anticancer activities were evaluated by MTT assay. Results: Twenty-seven derivatives have been synthesized in moderate to good yields. A number of derivatives exhibited potential antibacterial, antifungal and anticancer activities. Conclusion: Compounds (1b, 1e and 1g) showed antibacterial activity against Streptococcus faecalis, MSSA and MRSA with MIC ranging between 4 to 64 µg/mL. Compound (2g) showed antifungal activity against Candida albicans (8 µg/mL) and Aspergillus niger (64 µg/mL). Compound (1o) exhibited high cytotoxic activity against HepG2 cell line (IC50 value 8.6 µM), which is comparable to the activity of paclitaxel, and is non-toxic on LLC-PK1 normal cell line. The structure activity relationship and molecular docking study of the synthesized compounds are also reported.

(–)-Agelasidine A from Agelas clathrodes

2006 ◽  
Vol 61 (7-8) ◽  
pp. 472-476 ◽  
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.

scholarly journals Synthesis of Biogenic Silver Nanoparticles (AgCl-NPs) Using a Pulicaria vulgaris Gaertn. Aerial Part Extract and Their Application as Antibacterial, Antifungal and Antioxidant Agents

Nanomaterials ◽  
2020 ◽  
Vol 10 (4) ◽  
pp. 638 ◽  
Author(s):  
Majid Sharifi-Rad ◽  
Pawel Pohl
Keyword(s):  
Antioxidant Activity ◽  
Candida Albicans ◽  
Aerial Part ◽  
Silver Chloride ◽  
Radical Scavenging ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Antioxidant Agents ◽  
Vis Spectroscopy ◽  
Antibacterial And Antifungal

In this study, very simple and fast one-step synthesis of biogenic silver chloride nanoparticles (AgCl-NPs) using a Pulicaria vulgaris Gaertn. aerial part extract from an aqueous solution of silver nitrate at room temperature is proposed. The proceedings of the reaction were investigated by UV–Vis spectroscopy. AgCl-NPs were characterized using X-ray diffraction spectroscopy (XRD), Fourier-transform infrared spectroscopy (FTIR), and transmission electron microscopy (TEM). Antibacterial and antifungal activities of these nanoparticles were evaluated by disk diffusion and microdilution methods against Staphylococcus aureus, Escherichia coli, Candida albicans, and C. glabrata. In addition, the antioxidant activity of the synthesized AgCl-NPs was determined by the DPPH radical scavenging assay. The antimicrobial test confirmed the bactericidal activity of biosynthesized AgCl-NPs against Gram-positive and Gram-negative bacteria. They also exhibited good antifungal activities with minimum inhibitory concentration (MIC) values ranging from 40 to 60 µg/mL against Candida glabrata and Candida albicans, respectively. In addition, biosynthesized AgCl-NPs were established to have remarkable antioxidant activity. All this pointed out that the proposed new biosynthesis approach resulted in production of AgCl-NPs with convenient biomedical applications.

scholarly journals In VitroPhytochemical, Antibacterial, and Antifungal Activities of Leaf, Stem, and Root Extracts ofAdiantum capillus veneris

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Muhammad Saqib Ishaq ◽  
Muhammad Medrar Hussain ◽  
Muhammad Siddique Afridi ◽  
Ghadir Ali ◽  
Mahrukh Khattak ◽  
...  
Keyword(s):  
Multidrug Resistant ◽  
Antimicrobial Activities ◽  
Phytochemical Analysis ◽  
Bacterial Strains ◽  
Antifungal Activities ◽  
Fungal Strains ◽  
Antibacterial And Antifungal Activities ◽  
Adiantum Capillus Veneris ◽  
Ethanol Extracts ◽  
Antibacterial And Antifungal

Adiantum capillus venerisis a medicinally essential plant used for the treatment of diverse infectious diseases. The study of phytochemical and antimicrobial activities of the plant extracts against multidrug-resistant (MDR) bacteria and medically important fungi is of immense significance. Extracts from the leaves, stems, and roots ofAdiantum capillus veneriswere extracted with water, methanol, ethanol, ethyl acetate, and hexane and screened for their antimicrobial activity against ten MDR bacterial strains and five fungal strains isolated from clinical and water samples. Ash, moisture, and extractive values were determined according to standard protocols. FTIR (Fourier transform infrared Spectroscopy) studies were performed on different phytochemicals isolated from the extracts ofAdiantum capillus Veneris. Phytochemical analysis showed the presence of flavonoids, alkaloids, tannins, saponins, cardiac glycosides, terpenoids, steroids, and reducing sugars. Water, methanol, and ethanol extracts of leaves, stems, and roots showed significant antibacterial and antifungal activities against most of the MDR bacterial and fungal strains. This study concluded that extracts ofAdiantum capillus venerishave valuable phytochemicals and significant activities against most of the MDR bacterial strains and medically important fungal strains.

scholarly journals SYNTHESIS, CHARACTERIZATION AND IN VITRO STUDY OF ANTIBACTERIAL, ANTIFUNGAL ACTIVITIES OF SOME NOVEL DIHYDROPYRIMIDINTHIONE DERIVATIVES

2014 ◽  
Vol 44 (4) ◽  
pp. 289-293
Author(s):  
S. BALUJA ◽  
S. CHANDA ◽  
R. BHALODIA ◽  
R. TALAVIYA
Keyword(s):  
Biological Activities ◽  
Wide Spectrum ◽  
In Vitro Study ◽  
Dimethyl Formamide ◽  
Mass Spectral Data ◽  
Antifungal Activities ◽  
Mass Spectral ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

Dihydropyrimidinthione is an important class of heterocyclic compounds which exhibits wide spectrum of biological activities. In the present study, some bio-active dihydropyrimidinthione derivatives have been synthesized and their characterization was done by IR, NMR and mass spectral data. The antibacterial and antifungal activities of synthesized compounds have also been studied in N,N-dimethyl formamide and Dimethyl sulfoxide.

scholarly journals Synthesis, Characterization and Study of Antimicrobial Activities of Mannich Bases Incorporating 1,2,4-Triazole Nucleus

2021 ◽  
Vol 2 (01) ◽  
pp. 19-27
Author(s):  
Rhambus Rawat ◽  
Prem Shankar Deo ◽  
Bhushan Shakya
Keyword(s):  
Schiff Base ◽  
Heterocyclic Compounds ◽  
Environmental Science ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Mannich Bases ◽  
New Drugs ◽  
Spectroscopic Techniques ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

Heterocyclic compounds containing triazole moiety have great importance in the field of medicine, pharmaceuticals, biochemistry, biology, therapeutics, environmental science, and industry. Triazoles and their derivatives have been extensively used in the development of new drugs. Biological activities of Schiff bases are highly investigated, but Mannich bases are on the verge of their development, and they are being synthesized in large number nowadays. In this work, Mannich bases are synthesized by incorporation 1,2,4-triazole moiety through Schiff base using different amines. Mannich bases are found to exhibit highly effective antibacterial and antifungal activities. The formation of synthesized compounds - 1,2,4-triazole-5-thione, Schiff base (4) and Mannich bases (5a and 5b) - are confirmed and characterized by spectroscopic techniques like UV, FTIR 1H-NMR and 13C-NMR. The activity of the synthesized compounds was tested against bacterial and fungal strain.

scholarly journals Antibacterial Potential of Citral Derivatives

2011 ◽  
Vol 6 (9) ◽  
pp. 1934578X1100600
Author(s):  
Soni A. Singh ◽  
Yogesh A. Potdar ◽  
Rasika S. Pawar ◽  
Sujata V. Bhat
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Activities ◽  
Serial Dilution ◽  
Disc Diffusion ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal ◽  
Antibacterial Potential

Nine conjugated acid derivatives from monoterpene citral have been synthesized using ester, amide condensations, Wittig, Knoevenagel, Baylis-Hillman reactions and their antimicrobial activities were evaluated through disc diffusion and serial dilution methods. Several derivatives displayed interesting antimicrobial activity. Particularly, the Baylis-Hillman adducts 8-10 were found to have more potent antibacterial and antifungal activities than standard drugs namely chloramphenicol and nystatin respectively.

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