scholarly journals Synthesis, characterization and Cytotoxicity Evaluation of New Compounds from Oxazol-5(4H)-ones and Oxazoles Class Containing 4-(4-Bromophenylsulfonyl)phenyl Moiety

2019 ◽  
Vol 70 (4) ◽  
pp. 1099-1107
Author(s):  
Theodora-Venera Apostol ◽  
Stefania-Felicia Barbuceanu ◽  
Octavian Tudorel Olaru ◽  
Constantin Draghici ◽  
Gabriel Saramet ◽  
...  
Keyword(s):  
Acetic Anhydride ◽  
Phosphorus Oxychloride ◽  
Spectral Studies ◽  
Ethyl Chloroformate ◽  
Anhydrous Aluminum Chloride ◽  
1H And 13C Nmr ◽  
Ft Ir ◽  
Concentrated Sulfuric Acid ◽  
New Compounds

Steiger N-acylation of a-alanine with 4-(4-bromophenylsulfonyl)benzoyl chloride led to 2-[4-(4-bromophenylsulfonyl)benzamido]propanoic acid. This compound underwent intramolecular cyclization in the presence of N-methylmorpholine and ethyl chloroformate or acetic anhydride to the corresponding saturated azlactone. Then acylaminoacylation of dry aromatic hydrocarbons with 2-[4-(4-bromophenylsulfonyl)phenyl]-4-methyloxazol-5(4H)-one or 2-[4-(4-bromophenylsulfonyl) benzamido ]propanoyl chloride in the presence of anhydrous aluminum chloride led to corresponding a-acylamino ketones. These new intermediates were heterocyclized under the action of phosphorus oxychloride or concentrated sulfuric acid in the presence of acetic anhydride to the corresponding oxazoles. The newly synthesized compounds were characterized by spectral studies (FT-IR, UV-Vis, MS, 1H- and 13C-NMR) and elemental analysis. The purity of the new compounds was evaluated by RP-HPLC. The experimental research regarding to the in vitro cytotoxic activity of the new compounds were performed using Daphnia magna bioassay.

scholarly journals New Dihydroxytyrosyl Esters from Dicarboxylic Acids: Synthesis and Evaluation of the Antioxidant Activity In Vitro (ABTS) and in Cell-Cultures (DCF Assay)

Molecules ◽  
2020 ◽  
Vol 25 (14) ◽  
pp. 3135
Author(s):  
Elia Roma ◽  
Elena Mattoni ◽  
Paolo Lupattelli ◽  
Seyed Sepehr Moeini ◽  
Tecla Gasperi ◽  
...  
Keyword(s):  
Antioxidant Activity ◽  
Dicarboxylic Acids ◽  
Antioxidant Effect ◽  
Cosmetic Products ◽  
1H And 13C Nmr ◽  
New Class ◽  
Ft Ir ◽  
New Compounds ◽  
Very High

New dihydroxytyrosyl esters 2a, 2c–2j of dicarboxylic acids were synthesized from methyl orthoformate protected hydroxytyrosol 3 and diacyl chlorides. New compounds were characterized (HRMS, FT-IR, 1H- and 13C-NMR), and tested for antioxidant activity both in vitro (ABTS) and on L6 myoblasts and THP1 leukemic monocytes cell culture by DCF assay. According to the ABTS assay, compounds 2a, 2c–2j showed a TEAC value of antioxidant capacity up to twice that of Trolox. Very high or complete ROS protections were obtained in the cell environment where lipophilicity and rigidity of dicarboxylic structure seem to facilitate the antioxidant effect. MTT assay and proliferation test were used for assessment of cell viability. These compounds can be envisaged as a new class of preservatives for food or cosmetic products.

scholarly journals Microwave-Assisted Synthesis, Characterization, Antimicrobial and Antioxidant Activity of Some New Isatin Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
G. Kiran ◽  
T. Maneshwar ◽  
Y. Rajeshwar ◽  
M. Sarangapani
Keyword(s):  
Antioxidant Activity ◽  
Free Radical ◽  
Radical Scavenging ◽  
Microwave Assisted Synthesis ◽  
Stable Free Radical ◽  
Ft Ir ◽  
Antimicrobial And Antioxidant Activity ◽  
New Compounds ◽  
Isatin Derivatives

A series of β-Isatin aldehyde-N,N′-thiocarbohydrazone derivatives were synthesized and assayed for theirin vitroantimicrobial and antioxidant activity. The new compounds were characterized based on spectral (FT-IR, NMR, MS) analyses. All the test compounds possessed a broad spectrum of activity having MIC values rangeing from 12.5 to 400 μg/ml against the tested microorganisms. Among the compounds3e,3jand3nshow highest significant antimicrobial activity. The free radical scavenging effects of the test compounds against stable free radical DPPH (α,α-diphenyl-β-picryl hydrazyl) and H2O2were measured spectrophotometrically. Compounds3j,3n,3l, and3e, respectively, had the most effective antioxidant activity against DPPH and H2O2scavenging activity.

scholarly journals Synthesis, Characterization, and Antimicrobial Activity of Methyl-2-aminopyridine-4-carboxylate Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
S. Nagashree ◽  
P. Mallu ◽  
L. Mallesha ◽  
S. Bindya
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Studies ◽  
H Nmr ◽  
Chemical Structures ◽  
Elemental Analyses ◽  
Ft Ir

A series of methyl-2-aminopyridine-4-carboxylate derivatives,3a–f,were synthesized in order to determine theirin vitroantimicrobial activity. The chemical structures of the synthesized compounds were confirmed by elemental analyses, FT-IR, and1H NMR spectral studies. Among the synthesized compounds,3cand3dshowed good antimicrobial activity compared to other compounds in the series.

Synthesis,Characterization and Evaluation of Biological Activity of Sulfonylhydrazide-Schiff Base" (E)- N’-(2,5-dimethoxybenzalidene) naphthalene-2-sulfonohydrazide"

2020 ◽  
Vol 8 (1) ◽  
pp. 01-11
Author(s):  
Sameer Amereih ◽  
Abd Daraghmeh ◽  
Ismail Warad ◽  
Mohammed Al-Nuri
Keyword(s):  
Schiff Base ◽  
Inhibitory Concentration ◽  
Condensation Reaction ◽  
Gram Negative Bacteria ◽  
Biological Applications ◽  
Bacteriostatic Effect ◽  
1H And 13C Nmr ◽  
13C Nmr Analysis ◽  
Ft Ir

Condensation reaction of naphthalene -2-Sulfonylhydrazide, as starting material with 2,5-dimethoxy benzaldehyde was used to produce (E)-N’-(2,5-dimethoxybenzalidene)naphthalene-2-sulfonohydrazide. The Schiff base product was isolated, purified and then spectrally characterized via UV-Vis, GC/MS, FT-IR, 1H and 13C NMR analysis, where strong evidences confirmed the formation of the desired product. Antimicrobial activity of Schiff base product was evaluated in vitro against several types of bacteria such as: Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Klebsiella pneumoniae and MRSA by Minimum Inhibitory Concentration (MIC) test using tetracycline (TE) as a standard antibiotic. The tests showed a promising bacteriostatic effect of this compound against gram negative bacteria such as P. aeruginosa and K. pneumoniae, such character is valuable for biological applications.

Synthesis and DFT Studies of Pyrimidin-1(2H)-ylaminofumarate Derivatives

2020 ◽  
Vol 42 (5) ◽  
pp. 746-746
Author(s):  
Murat Saracoglu Murat Saracoglu ◽  
Zulbiye Kokbudak Zulbiye Kokbudak ◽  
M Izzettin Yilmazer and Fatma Kandemirli M Izzettin Yilmazer and Fatma Kandemirli
Keyword(s):  
Quantum Chemical ◽  
Energy Gap ◽  
Basis Set ◽  
Chemical Hardness ◽  
Pyrimidine Derivatives ◽  
1H And 13C Nmr ◽  
Solvent Phase ◽  
B3lyp Method ◽  
Ft Ir ◽  
New Compounds

Pyrimidine derivatives have biological and pharmacological properties. Therefore, in this study we focused on the synthesis various Pyrimidine derivatives to make noteworthy contributions this class of heterocyclic compounds. In the present study, the new compounds (4-6) were obtained by the reactions of 1-amino-5-benzoyl-4-phenylpyrimidin-2(1H)-one (1), 1-amino-5-(4-methylbenzoyl)-4-(4-methylphenyl)pyrimidin-2(1H)-one (2) and 1-amino-5-(4-methoxybenzoyl)-4-(4-methoxyphenyl)pyrimidin-2(1H)-one (3) with dimethyl acetylenedicarboxylate. The structures of these compounds were proved by elemental analysis, FT-IR, 1H and 13C-NMR spectra. In addition to, quantum chemical calculations were made to find molecular properties of the pyrimidin-1(2H)-ylaminofumarate derivatives (4-6) by using DFT/B3LYP method with 6-311++G(2d,2p) basis set. Quantum chemical features such as EHOMO, ELUMO, energy gap, ionization potential, chemical hardness, chemical softness, electronegativity etc. values for gas and solvent phase of neutral molecules were calculated and discussed.

Steroid Compounds Isolation from Carthamus tinctorius Linn as Antimalarial

2021 ◽  
pp. 5297-5304
Author(s):  
Rini Hamsidi ◽  
Wahyuni Wahyuni ◽  
Adryan Fristiohady ◽  
Muhammad Hajrul Malaka ◽  
Idin Sahidin ◽  
...  
Keyword(s):  
Antimalarial Activity ◽  
Carthamus Tinctorius ◽  
Spectroscopic Techniques ◽  
1H And 13C Nmr ◽  
Marker Compound ◽  
Ic50 Value ◽  
Ft Ir ◽  
Ir Spectroscopic

Carthamus tinctorius Linn, also known as safflower, is a plant with the potential of being used in the production of antimalarial drugs. The purpose of this study was to isolate and identify the steroid compounds in the safflower and determine its antimalarial activity in vitro. The isolation process was conducted through extraction and chromatography methods. Then, the characterization of the isolated compounds was conducted through spectroscopic techniques which include Fourier Transform Infrared Spectroscopy (FT-IR), NMR 1-D (1H and 13C-NMR), and NMR 2-D (HMQC, HMBC, and H-H COZY) as well as comparing data with the existing literatures. In addition, the tests conducted were with variations of isolate concentrations (10, 1, 0.1, 0.01, and 0.001 μg/mL) against 3D7 strain of Plasmodium falciparum. Based on the FT-IR spectroscopic data, the steroid compounds isolated from safflowers might be stigmasterols. In addition, the isolates had -OH functional group in the region of 3431 cm-1, C-O in the region of 1053 cm-1, and Csp3-H in regions of 2960, 2934, and 2865 cm-1. The NMR 1-D data showed presence of 29 carbon atoms, while the protons were 48 in number. Furthermore, the IC50 value of the compound was 34.03 μg/mL with a percentage inhibition of 43.92% against the growth of P. falciparum. Therefore, it was classified as inactive agent in inhibiting the growth of malaria parasites, however, it could be used as a marker compound in C. tinctorius Linn extract.

scholarly journals Synthesis and Characterization of 2-Pyrazoline Derivatives and their in silico and in vitro Studies on Antimicrobial and Anticancer Activities

2019 ◽  
Vol 31 (10) ◽  
pp. 2191-2196 ◽  
Author(s):  
S. Rathinamanivannan ◽  
K. Megha ◽  
Raja Chinnamanayakar ◽  
Ashok Kumar ◽  
M.R. Ezhilarasi
Keyword(s):  
Breast Cancer ◽  
Synthesis And Characterization ◽  
Anticancer Activities ◽  
1H And 13C Nmr ◽  
Chemical Structures ◽  
Ft Ir ◽  
Affinity Score ◽  
High Binding Affinity

The new series of 1-(4,5-dihydro-5-phenyl-3-diphenylpyrazol-1-yl)butan-1-one derivatives were synthesized by cyclization method using biphenyl chalcone with n-butyric acid and hydrazine hydrate. The synthesized 1-(4,5-dihydro-5-phenyl-3-diphenylpyrazol-1-yl)butan-1-one derivatives chemical structures were confirmed from spectral data such as FT-IR, 1H and 13C NMR. 2-Pyrazoline derivatives were docked with bacterial (1UAG) and breast cancer (1OQA) protein. Based on high binding affinity score, the best compound was subjected to in vitro anticancer activity by MTT assay. Also, antimicrobial activity were studied for synthesized 2-pyrazoline derivatives.

scholarly journals Synthesis of 1-(4-phenoxyphenyl)-3-[5-(substituted aryl)-1,3,4-oxadiazol-2-yl]propan-1-ones as safer anti-inflammatory and analgesic agents

2008 ◽  
Vol 73 (8-9) ◽  
pp. 781-791 ◽  
Author(s):  
Asif Husain ◽  
F.J. Ahmad ◽  
Mohd Ajmal ◽  
Priyanka Ahuja
Keyword(s):  
Lipid Peroxidation ◽  
Phosphorus Oxychloride ◽  
1H And 13C Nmr ◽  
Writhing Test ◽  
Rat Paw Edema ◽  
Malondialdehyde Content ◽  
Analgesic Agents ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
New Compounds

A novel series of 1-(4-phenoxyphenyl)-3-[5-(substituted aryl)-1,3,4-oxa- diazol-2-yl]propan-1-one was synthesized by reaction of 3-(4-phenoxybenzoyl)propionic acid with several aryl acid hydrazides in phosphorus oxychloride. The structures of the compounds were supported by IR, 1H- and 13C-NMR, MS data and elemental analysis results. These compounds were tested for their anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation actions. A few compounds were found to have very good anti-inflammatory activity in the carrageenan-induced rat paw edema test, while a fair number of the compounds showed significant analgesic activity in the acetic acid-induced writhing test. These new compounds showed very low ulcerogenic action with reduced malondialdehyde content (MDA), which is one of the by-products of lipid peroxidation.

scholarly journals Synthesis, Antimicrobial Screening, Homology Modeling, and Molecular Docking Studies of a New Series of Schiff Base Derivatives as Prospective Fungal Inhibitor Candidates

Molecules ◽  
2019 ◽  
Vol 24 (18) ◽  
pp. 3250 ◽  
Author(s):  
Yahya Toubi ◽  
Farid Abrigach ◽  
Smaail Radi ◽  
Faiza Souna ◽  
Abdelkader Hakkou ◽  
...  
Keyword(s):  
Schiff Base ◽  
Homology Modeling ◽  
Condensation Reaction ◽  
Docking Studies ◽  
Antifungal Effect ◽  
1H And 13C Nmr ◽  
Schiff Base Derivatives ◽  
Ft Ir ◽  
Antibacterial And Antifungal

Twelve new Schiff base derivatives have been prepared by the condensation reaction of different amino substituted compounds (aniline, pyridin-2-amine, o-toluidine, 2-nitrobenzenamine, 4-aminophenol, and 3-aminopropanol) and substituted aldehydes such as nicotinaldehyde, o,m,p-nitrobenzaldehyde, and picolinaldehyde in ethanol using acetic acid as a catalyst. The envisaged structures of the all the synthesized ligands have been confirmed on the basis of their spectral analysis FT-IR, mass spectroscopy, 1H- and 13C-NMR. In vitro screening of their antibacterial and antifungal potential against Escherichia coli bacterium and Fusarium oxysporum f.sp albedinis (F.o.a) fungus, respectively, revealed that all the ligands showed no significant antibacterial activity, whereas most of them displayed good antifungal activity. Homology modeling and docking analysis were performed to explain the antifungal effect of the most and least active compound against two F.o.a fungus proteins.

scholarly journals Synthesis, antimicrobial and antimalarial activityof1, 4-benzothiazepine and pyrazolinederivatives incorporating carbazolemoiety

2019 ◽  
Vol 51 (2) ◽  
pp. 234-241
Author(s):  
V. A. Kadnor ◽  
S. N. Shelke
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
13C Nmr ◽  
Antimalarial Activity ◽  
Positive Control ◽  
Spectral Studies ◽  
Standard Drug ◽  
Mass Spectral ◽  
Ft Ir

A series of carbazole-based 1,4-benzothiazepine and pyrazoline derivatives were synthesized and the structures of the newly synthesized compounds were confirmed by FT-IR, 1H NMR, 13C NMR and mass spectral studies. All new derivatives 4(a-f) and 5(a-e) were screened for their in vitro antimicrobial activity, and also for their antimalarial activity. Compounds 4a, 4b, 4d, 5a, 5b and 5c exhibited promising antimicrobial and antimalarial activities as compared to positive control. Notably, compounds 4a, 4b and 4d showed excellent antifungal activity against Penicillium sp. comparable to that of a standard drug.

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