scholarly journals Synthesis, antimicrobial and antiradical activity of (3-alkoxymethyl-4-hydroxyphenyl)propan-1-ones, intermediates of biologically active compounds and activity comparison with 3-(alkoxymethyl)-4-(alkylamino-2-hydroxypropoxyphenyl)alkanones type of beta blockers

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
R. Čižmáriková ◽  
M. Markuliak ◽  
L. Habala ◽  
J. Valentová ◽  
A. Bilková
Keyword(s):  
Biological Activities ◽  
Beta Blockers ◽  
Antimicrobial Activities ◽  
Biologically Active ◽  
Human Pathogens ◽  
Positive Bacterium ◽  
H Nmr ◽  
Hydrogen Carbonate ◽  
Activity Comparison ◽  
C Nmr

Abstract A homologous series of (3-alkoxymethyl-4-hydroxyphenyl)propan-1-ones was prepared by the reaction of (3-chloromethyl-4-hydroxyphenyl)propan-1-ones with the corresponding alcohols (methanol – decan-1-ol, propan-2-ol, 2-methylpropan-1-ol, 3-methylbutan-1-ol, cyclopentanol, benzylalcohol) in the presence of sodium hydrogen carbonate. The composition of the synthesised compounds was elucidated by IR, UV and 1H-NMR and 13C-NMR spectra. Selected compounds were tested against human pathogens: gram-positive bacterium Staphylococcus aureus (CNCTC Mau 29/58), gram-negative bacterium Escherichia coli (CNCTC 377/79) and yeast Candida albicans (CCM 8186). Their antimicrobial activities were expressed as minimum inhibitory concentrations. Antioxidant activity was determined using DPPH and ABTS.+ methods. It could be shown that both biological activities, antimicrobial and antioxidant, were lower in comparison with the (2RS)-bis [3-(4-acetyl-2-propoxymethyl)phenoxy-2-hydroxypropyl]isopropylammonium fumarate type of beta blockers.

scholarly journals Design and synthesis of a novel 5-(aminomethylene)thiazolidine-2,4-dione derivatives as potent hepatitis-B virus polymerase inhibitors

2015 ◽  
Vol 10 (2) ◽  
pp. 271
Author(s):  
Wei-Guo Li ◽  
He-Qun Wang
Keyword(s):  
Hbv Dna ◽  
Biologically Active ◽  
Secondary Amines ◽  
Design And Synthesis ◽  
H Nmr ◽  
Viral Antigens ◽  
Polymerase Inhibitors ◽  
Potent Inhibition ◽  
B Virus ◽  
C Nmr

<p>A series of novel thiazolidinedione analogues (TZD) were designed and synthesized potent inhibitors of HBV capsid assembly. The synthesis of thiazolidine-2,4-dione derivatives (4a–4o), starting from the condensation of 5-(ethoxymethylene)thiazolidine-2,4-dione (1) with various secondary amines (3) derived from biologically active compounds. The newly synthesized TZD analogues 4a-4o were characterized by <sup>1</sup>H NMR, <sup>13</sup>C NMR, and MS and evaluated for their anti-HBV activity. Most of the compounds inhibited the expression of viral antigens at low concentration. Six compounds, 4g, 4h, 4l, 4m, 4n, and 4o, demonstrated potent inhibition of HBV DNA replication at submicromolar range. Of these five initial hits, compound 4o was the most active when compared with lamivudine.</p><p> </p><p> </p>

scholarly journals Synthesis, Characterization, and Agricultural Biological Activities of 5-Fluoro-2-hydroxy Butyrophenone

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Fengli Xin ◽  
Chunhua Du ◽  
Gongjia Lan ◽  
Zhuanping Wu
Keyword(s):  
Lactuca Sativa ◽  
Biological Activities ◽  
Raw Material ◽  
Synthetic Approach ◽  
Target Compound ◽  
Echinochloa Crusgalli ◽  
Agricultural Plant ◽  
H Nmr ◽  
Valsa Mali ◽  
C Nmr

A novel synthetic approach towards 5-fluoro-2-hydroxy butyrophenone is reported. Using 4-fluorophenol as a raw material, the processes of etherification protection, Friedel-Crafts acylation and demethylation provide the target compound under mild conditions. The structure was characterized by the melting point and IR, MS,1H-NMR, and13C-NMR spectroscopy. The bioassay results indicate that the target compound exhibits potent antifungal activities againstValsa mali,Coniella dipodiella, and other agricultural plant fungi. The target compound also shows potent herbicidal activities forLactuca sativa, a dicotyledon, andEchinochloa crus-galli, a monocotyledon. The toxicity regression C50values of the compound againstValsa mali,Coniothyrium diplodiella,Lactuca sativaseedling, andEchinochloa crusgalliseedling were calculated by SPSS. The Hormesis effect for roots ofEchinochloa crusgalliwas confirmed.

scholarly journals Phytochemical Characterization and Evaluation of Biological Activities of Egyptian Carob Pods (Ceratonia siliqua L.) Aqueous Extract: In Vitro Study

Plants ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 2626
Author(s):  
Wael Sobhy Darwish ◽  
Abada El Sayed Khadr ◽  
Maher Abd El Naby Kamel ◽  
Mabrouk A. Abd Eldaim ◽  
Ibrahim El Tantawy El Sayed ◽  
...  
Keyword(s):  
Aqueous Extract ◽  
Biological Activities ◽  
Radical Scavenging ◽  
Antimicrobial Activities ◽  
Biologically Active ◽  
Phytochemical Analysis ◽  
Type I ◽  
Hypotonic Solution ◽  
Ceratonia Siliqua

Ceratonia siliqua (Carob) is an evergreen Mediterranean tree, and carob pods are potentially nutritive and have medicinal value. The present study was carried out to estimate the possible biological activities of phytochemical-characterized carob pod aqueous extract (CPAE). The phytochemical contents of CPAE were determined by using colorimetric methods and HPLC. In addition, the free radical scavenging properties and anti-diabetic, anti-hemolytic, and antimicrobial activities were estimated by using standardized in vitro protocols. The phytochemical analysis revealed that CPAE was rich in polyphenols, flavonoids, and alkaloids, where it contained a significant amount of gallic acid, catechin, and protocatechuic acid. Furthermore, CPAE exhibited strong antioxidant activity where it prevented the formation of 2, 2-Diphenyl-1-picryl hydrazyl, hydroxyl, and nitric oxide free radicals. Additionally, it had a potent inhibitory effect against digestive enzymes (amylase, maltase, sucrase, and lactase). Moreover, CPAE exhibited anti-Staph aureus, anti-Escherichia coli, anti-Candida albicans, and anti-herpes simplex type I virus (HSV-I). Finally, CPAE protected the erythrocyte membrane from hypotonic solution-induced hemolysis. Altogether, CPAE could be regarded as an interesting source of biologically active antioxidant, anti-diabetic, and antimicrobial preparation for a potential application in pharmaceutical and food supplement fields.

Synthesis and Characterization of a New Coumarin-1,2,3-Triazole Diad

2014 ◽  
Vol 618 ◽  
pp. 170-174
Author(s):  
Hong Qi Li ◽  
Xiu Juan Tian ◽  
Zhen Chen ◽  
Ding Xiao ◽  
Ning Fang ◽  
...  
Keyword(s):  
Click Chemistry ◽  
Biological Activities ◽  
Antitubercular Activity ◽  
Synthesis And Characterization ◽  
Target Compound ◽  
H Nmr ◽  
Mild Conditions ◽  
Ideal Approach ◽  
C Nmr

A new coumarin-1,2,3-triazole diad was designed and synthesized by Pechmann-Duisberg reaction and click chemistry. The three-step synthetic route to the target compound afforded an overall yield of 56%. The structures of the synthesized compounds were characterized by 1H NMR, 13C NMR, IR and mass spectrum. The click chemistry provided an ideal approach for synthesis under mild conditions of coumarin-1,2,3-triazole diads which may exhibit excellent biological activities such as antitubercular activity.

scholarly journals Synthesis and Spectroscopic Characterization of Some New Axially Ligated Indium(III) Macrocyclic Complexes and Their Biological Activities

2014 ◽  
Vol 2014 ◽  
pp. 1-7
Author(s):  
Gauri D. Bajju ◽  
Altaf Ahmed ◽  
Deepmala Gupta ◽  
Ashu Kapahi ◽  
Gita Devi
Keyword(s):  
Biological Activities ◽  
Spectroscopic Characterization ◽  
Axial Ligand ◽  
Free Base ◽  
H Nmr ◽  
Pyramidal Geometry ◽  
The Stability ◽  
Square Pyramidal Geometry ◽  
C Nmr

The synthesis and spectroscopic characterization of new axially ligated indium(III) porphyrin complexes were reported. Chloroindium(III) porphyrin (TPPIn-Cl) was obtained in good yield by treating the corresponding free base with indium trichloride. The action of the different phenols on chloroderivatives (TPPIn-Cl) led to the corresponding phenolato complexes (TPPIn-X). These derivatives were characterized on the basis of mass spectrometry,1H-NMR, IR, and UV-visible data. The separation and isolation of these derivatives have been achieved through chromatography. The spectral properties of free base porphyrin and its corresponding metallated and axially ligated indium(III) porphyrin compounds were compared with each other. A detailed analysis of UV-Vis,1H-NMR, and IR suggested the transformation from free base porphyrin to indium(III) porphyrin. Besides,13C-NMR and fluorescence spectra were also reported and interpreted. The stability of these derivatives has also been studied through thermogravimetry. The complexes were also screened for anticancerous activities. Among all the complexes, 4-MePhO-InTPP shows highest anticancerous activity. The title complexe, TPPIn-X (where X = different phenolates), represents a five-coordinate indium(III) porphyrin complex in a square-pyramidal geometry with the phenolate anion as the axial ligand.

Synthesis and Biological Activities of Some Schiff's Bases from 4-amino-3-(3-hydroxybutyl)-1H-1, 2, 4-triazole-5-thione

2009 ◽  
Vol 2009 (4) ◽  
pp. 208-211 ◽  
Author(s):  
Jing Zhang ◽  
Lixue Zhang ◽  
Xinxiang Lei ◽  
Changfeng Zhou ◽  
Xiaodan Fu ◽  
...  
Keyword(s):  
Plant Growth ◽  
Elemental Analysis ◽  
Mass Concentration ◽  
Biological Activities ◽  
Schiff’S Bases ◽  
H Nmr ◽  
Schiff's Bases ◽  
High Yields ◽  
C Nmr ◽  
Growth Regulating Activity

Sixteen novel Schiff's bases have been synthesised in high yields from 4-amino-3-(3-hydroxybutyl)-1 H-1, 2, 4-triazole-5-thione. All the newly synthesised compounds have been characterised by elemental analysis, IR, 1H NMR, 13C NMR and MS. Plant growth-regulating activity tests showed that most compounds have remarkable effects on the growth of wheat and radish at a mass concentration of 50μg mL−1.

scholarly journals Antimicrobial Applications of Transition Metal Complexes of Benzothiazole Based Terpolymer: Synthesis, Characterization, and Effect on Bacterial and Fungal Strains

2014 ◽  
Vol 2014 ◽  
pp. 1-16 ◽  
Author(s):  
Mohamed A. Riswan Ahamed ◽  
Raja S. Azarudeen ◽  
N. Mujafar Kani
Keyword(s):  
Metal Complexes ◽  
Elemental Analysis ◽  
Biological Activities ◽  
Gel Permeation Chromatography ◽  
Spectral Studies ◽  
X Ray Diffraction ◽  
Spectral Techniques ◽  
H Nmr ◽  
Uv Visible ◽  
C Nmr

Terpolymer of 2-amino-6-nitro-benzothiazole-ethylenediamine-formaldehyde (BEF) has been synthesized and characterized by elemental analysis and various spectral techniques like FTIR, UV-Visible, and1H and13C-NMR. The terpolymer metal complexes were prepared with Cu2+, Ni2+, and Zn2+metal ions using BEF terpolymer as a ligand. The complexes have been characterized by elemental analysis and IR, UV-Visible, ESR,1H-NMR, and13C-NMR spectral studies. Gel permeation chromatography was used to determine the molecular weight of the ligand. The surface features and crystalline behavior of the ligand and its complexes were analyzed by scanning electron microscope and X-ray diffraction methods. Thermogravimetric analysis was used to analyze the thermal stability of the ligand and its metal complexes. Kinetic parameters such as activation energy(Ea)and order of reaction (n) and thermodynamic parameters, namely,ΔS,ΔF,S*, andZ, were calculated using Freeman-Carroll (FC), Sharp-Wentworth (SW), and Phadnis-Deshpande (PD) methods. Thermal degradation model of the terpolymer and its metal complexes was also proposed using PD method. Biological activities of the ligand and its complexes were tested againstShigella sonnei,Escherichia coli,Klebsiellaspecies,Staphylococcus aureus,Bacillus subtilis, andSalmonella typhimuriumbacteria andAspergillus flavus,Aspergillus niger,Penicilliumspecies,Candida albicans,Cryptococcus neoformans,Mucor speciesfungi.

scholarly journals Novel 5,6-Dihydropyrrolo[2,1-a]isoquinolines as Scaffolds for Synthesis of Lamellarin Analogues

2011 ◽  
Vol 2011 ◽  
pp. 1-6 ◽  
Author(s):  
Shao Han Liao ◽  
Dai Hua Hu ◽  
Ai Ling Wang ◽  
De Peng Li
Keyword(s):  
Melting Point ◽  
Ir Spectrum ◽  
Biological Activities ◽  
Synthetic Route ◽  
H Nmr ◽  
C Nmr

As core skeletons of lamellarins: 5,6-Dihydropyrrolo[2,1-a]isoquinolines are one of the important alkaloids that exhibit significant biological activities, in this study, an efficient synthetic route was described for two novel compounds, 5,6-dihydropyrrolo[2,1-a]isoquinolinesIandII. CompoundIwas synthesized from isovanillin with 28.3% overall yield by a six-step reaction whileIIfrom 2-(3,4-dimethoxyphenyl) ethanamine was with 61.6% overall yield by a three-step reaction. And the structures of these two compounds were confirmed by means of IR spectrum,1H NMR,13C NMR, MS, HRMS, and melting point measurements.

scholarly journals Synthesis and Characterization of Novel 1,3-Thiazole and 2-Amino-1,3,4-Thiadiazole Derivatives

2014 ◽  
Vol 33 (2) ◽  
pp. 189 ◽  
Author(s):  
Mustafa Er ◽  
Ayşe Şahin ◽  
Hakan Tahtacı
Keyword(s):  
Biological Activities ◽  
High Yield ◽  
Synthesis And Characterization ◽  
Hantzsch Reaction ◽  
H Nmr ◽  
Thiadiazole Derivatives ◽  
High Yields ◽  
Mass Spectrometric Techniques ◽  
C Nmr

<p>Thiosemicarbazone derivatives <strong>3a–e</strong> were synthesized by the reaction of various aldehydes<strong> 1a–e</strong> with 4-methyl thiosemicarbazide <strong>2</strong> in 78% to 90% yield. Then, the thiazole moieties of the target materials <strong>5a–e</strong> were obtained in high yields (71–93%) using the Hantzsch reaction utilizing thiosemicarbazone derivatives <strong>3a–e</strong> with ethyl-2-chloroacetoacetic ester. The substituted nitrile derivatives <strong>7a–e</strong> were obtained in moderate to high yield (58–84%) from the reaction of compounds <strong>5a–e</strong> with chloroacetonitrile by the nucleophilic aliphatic substitution reaction in the presence of anhydrous potassium carbonate. Finally, substituted 2-amino-1,3,4-thiadiazole compounds <strong>9a–e</strong> were obtained in moderate to good yields (51–62%) from the reaction of thiosemicarbazide with substituted nitrile derivatives <strong>7a–e</strong>. As a result, compounds that all share a high disposition for biological activities were obtained. The structures of the newly synthesized compounds were confirmed by IR, <sup>1</sup>H NMR, <sup>13</sup>C NMR, elemental analysis, and mass spectrometric techniques.</p>

scholarly journals Determination of Molecular Weight and Antimicrobial Activities of a Purified Bacteriocin from Lactiplantibacillus plantarum MDP 5

2021 ◽  
Vol 14 (4) ◽  
pp. 1600-1606
Author(s):  
T Punithavalli
Keyword(s):  
Molecular Weight ◽  
Dry Weight ◽  
Antimicrobial Activities ◽  
Hplc Method ◽  
Probiotic Bacterium ◽  
Biologically Active ◽  
Precipitation Method ◽  
Lactobacillus Species ◽  
Human Pathogens

Nowadays, unlimited use of antibiotics and preservatives have become a big concern regarding the human health which turn the interest of biotech industries into their research on biologically active molecules from probiotic microbes, since they are nontoxic and suitable for many safer applications. On this background, the present investigation focused on the characterization of a bacteriocin from a Lactobacillus strain. The characterization of a bacteriocin was done using a Lactiplantibacillus plantarum MDP 5 isolated from the local markets of Puducherry and production was performed under standardized cultural conditions. The study on the maximum recovery of bacteriocin using ammonium sulphate precipitation method revealed that the 60% saturation rate evidenced highest activity of 6500 AU/ml with 4.113g/L dry weight followed by the purification was done with RP-HPLC method using C18 column. The purified bacteriocin revealed a novel molecular weight of 22 kDa with the help of SDS-PAGE which has not been reported from Lactobacillus species. Further, the purified bacteriocin evidenced appreciable antimicrobial activities against all the tested human bacterial pathogens of this study. The highest antimicrobial activity was recorded against Escherichia coli MTCC 443 followed by Staphylococcus aureus MTCC 96, Vibrio parahemolyticus MTCC 451, Enterococcus faecalis MTCC 9845, Pseudomonas aeruginosa MTCC 741 and Klebsiella pneumoniae MTCC 109 in the concentrations of 8AU/ml, 16AU/ml, 32AU/ml, 64AU/ml, 256AU/ml and 512AU/ml, respectively. From the overall observation, this study explored a novel bacteriocin purified from a probiotic bacterium represented potential antimicrobial activities against many human pathogens which suggesting its possible use for the safe therapeutic applications.

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