CONVENTIONAL AND MICROWAVE SYNTHESIS AND ANTIOXIDANT EVALUATION OF BENZOTHIAZOLE SUBSTITUTED 4-THIAZOLIDINONES

INDIAN DRUGS ◽  
2021 ◽  
Vol 57 (10) ◽  
pp. 17-22
Author(s):  
Chaithra R Shetty ◽  
Ishwar K Bhat ◽  
Abhishek Kumar ◽  
Vijay Kumar Merugumolu ◽  
Revanasidappa BC ◽  
...  
Keyword(s):  
Thioglycolic Acid ◽  
Antioxidant Activities ◽  
Aromatic Aldehydes ◽  
Vital Role ◽  
Scientific Data ◽  
Hybrid Molecule ◽  
H Nmr ◽  
Antioxidant Evaluation

Antioxidants exert their action chiefly in controlling and preventing the free-radicals and their reactions and thus it has a vital role as health protecting factor. There are many scientific data proposing that antioxidants lower the threats of some chronic diseases including cancer and heart disease. In the present work, the hybrid molecule i.e benzothiazole substituted 4-thiazolidinone, has been taken for the study and different novel benzothiazole substituted 4-thiazolidinone derivatives were synthesized by reacting 2-amino-6-methyl benzothiazole with aromatic aldehydes in alcohol media. The resulting Schiff bases were made to react with thioglycolic acid in dioxane. Characterization of synthesized compounds was done by IR, 1 H NMR and Mass spectroscopy. The same reaction was performed in the microwave assisted reaction condition and compared with conventional synthesis. In vitro antioxidant activities of compounds were performed by three different methods, out of which Compound TZ4 emerged as a promising molecule.

Design, Synthesis, Characterization, Anti-Inflammatory and Antioxidant Evaluation of Certain Novel Pyrazoline Derivatives Containing Imidazo[2,1-b]thiazole Moiety

2020 ◽  
Vol 5 (1) ◽  
pp. 45-50
Author(s):  
V.D. Sonawane ◽  
B.D. Sonawane ◽  
M.J. Dhanavade ◽  
K.D. Sonawane ◽  
R.B. Bhosale
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Activities ◽  
Design Synthesis ◽  
Standard Drug ◽  
Drug Designing ◽  
Antioxidant Evaluation ◽  
Future Drug ◽  
Anti Inflammatory

In present study, a novel series of substituted imidazo[2,1-b]thiazole pyrazoline derivatives (2a-e) and (3a-e) from the reference compound imidazo[2,1-b]thiazole chalcones (1a-e) in PEG-400 by using hydrazine hydrate and phenyl hydrazine was synthesized. Characterization of newly synthesized compounds was done using IR and 1H NMR. Further, imidazo[2,1-b]thiazole pyrazoline derivatives were subjected to check their in vitro antioxidant activities at a concentration of 0.5 mmol/L in methanol. Compounds 2c, 2d, 3c, 3d and 3e showed comparatively good activity than standard drug diclofenac. The anti-inflammatory activity of compounds 2c, 2d, 2e, 3c, 3d and 3e were comparable with standard drug. Similarly, all these compounds possess good antioxidant activity as compared to ascorbic acid (vitamin C); compared to the value of DPPH and SOD antioxidant activity 44.18 % and 74.07 %, respectively. These synthesized compounds exhibited a good anti-inflammatory and antioxidant activities hence might be useful in future drug designing studies.

scholarly journals Synthesis and In Vitro Antioxidant Evaluation of Some Novel 4, 5-Dihydro-1H, 2, 4-triazol-5-one Derivatives

2010 ◽  
Vol 7 (1) ◽  
pp. 123-136 ◽  
Author(s):  
O. Gursoy Kol ◽  
H. Yuksek
Keyword(s):  
Spectral Data ◽  
Antioxidant Activities ◽  
Iron Binding ◽  
Acidic Properties ◽  
H Nmr ◽  
Elemental Analyses ◽  
Antioxidant Evaluation ◽  
C Nmr

In this study, thirteen novel 4,5-dihydro-1H-1,2,4-triazol-5-one derivatives were synthesized and characterized by elemental analyses and IR,1H NMR,13C NMR and UV spectral data. The synthesized compounds were analyzed for theirin vitropotential antioxidant activities in three different methods. Those antioxidant activities were compared to standard antioxidants such as BHA, BHT andα-tocopherol. The data reveal that the compounds demonstrate a marked capacity for iron binding, especially5aand7cIn addition to this, the compounds4were titrated potentiometrically with TBAH in non-aqueous solvents because of the weak acidic properties of 4,5-dihydro-1H-1,2,4-triazol-5-one ring N-H group.

scholarly journals Synthesis and In Vitro Antioxidant Evaluation of New 1,3,5-Tri-{2-methoxy-4-[(4,5-dihydro-1H-1,2,4-triazol-5-on-4-yl)-azomethine]-phenoxycarbonyl}-Benzene Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
H. Yuksek ◽  
O. Akyildirim ◽  
O. Gursoy Kol
Keyword(s):  
Isopropyl Alcohol ◽  
Antioxidant Activities ◽  
Butyl Alcohol ◽  
Dimethyl Formamide ◽  
Neutralization Potential ◽  
H Nmr ◽  
Elemental Analyses ◽  
Antioxidant Evaluation ◽  
C Nmr

Nine new 4,5-dihydro-1H-1,2,4-triazol-5-one derivatives were synthesized and characterized by elemental analyses and IR,1H-NMR,13C-NMR and UV spectral data. The synthesized compounds were analyzed for theirin vitropotential antioxidant activities in three different methods. Those antioxidant activities were compared to standard antioxidants such as BHA, BHT andα-tocopherol. Compounds4e,5aand5dshowed best activity for iron binding. In addition, the compounds4were titrated potentiometrically with tetrabutylammonium hydroxide (TBAH) in four non-aqueous solvents (isopropyl alcohol,tert-butyl alcohol, acetone andN,N-dimethyl formamide). Thus, the half-neutralization potential values and the correspondingpKavalues were determined in all cases.

scholarly journals Synthesis characterization and antibacterial studies of 4-aminoantipyrine schiff’s bases

2017 ◽  
Vol 2 (01) ◽  
pp. 8-14 ◽  
Author(s):  
K Sunand ◽  
K Vinay Kumar ◽  
K Ashwini ◽  
P Suresh Kumar ◽  
S Vishnu ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Schiff Bases ◽  
Vital Role ◽  
Spectroscopic Techniques ◽  
Schiff’S Bases ◽  
Pharmacological Activities ◽  
Schiff's Bases ◽  
Ir Spectroscopic

Aim: To synthesize and evaluate 4-aminoantipyrine related schiff’s bases as antibacterial agents. Objective: To synthesize, purify, characterize and evaluate 4-aminoantipyrine. Method: Schiff bases derived from 4-aminoantipyrine play a vital role in biological and pharmacological activities. Knowing the importance of 4-aminoatipyrine schiff bases and their analogues wide varieties of bioactivities like analgesic, antiviral, antipyretic, anti-rheumatic, antimicrobial and anti-inflammatory activities have been widely studied. 4-aminoantipyrine compounds C1 (anisaldehyde), C2 (p-hydroxybenzaldehyde) and C3(vanillin) were prepared by condensation between 4-amino antipyrine and substituted aromatic benzaldehydes. The products were purified by recrystallization by using ethanol, characterized by IR spectroscopy. The N-H stretching in 4-aminoantipyrine is shown at 3430 cm-1 and -3325 cm-1. The -HC=N- stretching is observed in the range of 1508-1504 cm-1 The –OCH3 stretching is found at 1888 cm-1. 4-amino antipyrine related schiff’s bases evaluated their activity as antimicrobials in-vitro by spread plate method against E.coli. Schiff bases have potent antibacterial activity with gram negative bacteria E.coli. Results: Synthesis and characterization of a schiff bases derived from substituted benzaldehydes and 4-aminoantipyrine was evaluated and characterized with the IR spectroscopic techniques and schiff bases have shown potent antibacterial activity against E.Coli.

PREPARATION AND CHARACTERIZATION OF GLYCYRRHETINIC ACID-MODIFIED POLOXAMER 188/CHITOSAN NANOPARTICLES

NANO ◽  
2013 ◽  
Vol 08 (04) ◽  
pp. 1350042 ◽  
Author(s):  
JING WANG ◽  
LI GUO ◽  
LI FANG MA
Keyword(s):  
High Performance ◽  
Drug Loading ◽  
Chitosan Nanoparticles ◽  
Spherical Shape ◽  
Glycyrrhetinic Acid ◽  
Poloxamer 188 ◽  
H Nmr ◽  
Ft Ir

In this paper, we firstly synthesized glycyrrhetinic acid-modified double amino-terminated poloxamer 188 (GA–NH–POLO–NH–GA). The structure of the synthesized compound was confirmed by 1H-NMR and Fourier transform infrared (FT-IR) spectroscopy. Then the nanoparticles composed of GA–NH–POLO–NH–GA/chitosan (GA–NH–POLO–NH–GA/CTS) were prepared by an ionic gelation process. The characterization of the nanoparticles was measured by dynamic light scattering (DLS) and scanning electron microscope (SEM). The results showed that the nanoparticles were well dispersed with a spherical shape and the particle size was distributed between 100 nm and 300 nm. The cytotoxicity based on MTT assay against cells (QGY-7703 cells and L929 cells) showed that the nanoparticles had low toxicity and good biocompatibility. The encapsulation efficiency and drug loading of 5-fluorouracil-loaded nanoparticles (5-FU nanoparticles) were measured by high-performance liquid chromatography (HPLC) and fluorescence spectroscopy, ultraviolet-visible (UV-vis) absorbance. The encapsulation of 5-Fu-loaded CTS nanoparticles was 12.8% and the drug loading was 2.9%, while the encapsulation of 5-Fu-loaded GA–NH–POLO–NH–GA/CTS nanoparticles was 20.9% and the drug loading was 3.36%. The release profile showed that the GA–NH–POLO–NH–GA/CTS nanoparticles were available for sustained release of 5-Fu. The GA–NH–POLO–NH–GA/CTS nanoparticles have a higher affinity to the QGY-7703 cells, so indicated that the GA–NH–POLO–NH–GA/CTS nanoparticles have the capacity of liver-targeting in vitro.

scholarly journals Synthesis and Optoelectronic Characterization of Some Star-Shaped Oligomers with Benzene and Triphenylamine Cores

2012 ◽  
Vol 2012 ◽  
pp. 1-11 ◽  
Author(s):  
Teofilia Ivan ◽  
Loredana Vacareanu ◽  
Mircea Grigoras
Keyword(s):  
Electrochemical Polymerization ◽  
Coupling Reaction ◽  
Aromatic Aldehydes ◽  
Thermal Characterization ◽  
Cyclic Voltammograms ◽  
Heck Coupling ◽  
Molecular Glasses ◽  
H Nmr ◽  
Ft Ir

Six star-shaped oligomers containing triphenylamine (D1–D3) and benzene unit (D4–D6) as cores have been synthesized by Wittig condensation or Heck coupling reaction using aromatic aldehydes and triphenylphosphonium salts or aromatic halogenated compounds with vinyl triphenylamine. All oligomers have well-defined molecular structure and high purity. Characterization of the oligomers was made by FT-IR, 1H-NMR spectroscopy, UV-Vis, and fluorescence spectroscopy. The electrochemical behavior was studied by cyclic voltammetry (CV). The cyclic voltammograms have revealed that oligomers undergo quasireversible or irreversible redox processes. The irreversible process is associated with electrochemical polymerization of oligomers by dimerization of unsubstituted triphenylamine groups. Thermal characterization was accomplished by TGA and DSC methods and evidenced that all oligomers were stable materials until 250°C and have formed stable molecular glasses after first heating scan.

Synthesis and Characterization of Polyesters Containing 5-Fluorouracil in the Main Chain

2012 ◽  
Vol 499 ◽  
pp. 99-103
Author(s):  
Jun Chang ◽  
Cheng Wu Li ◽  
Gang Li
Keyword(s):  
Main Chain ◽  
Slow Release ◽  
Uv Spectroscopy ◽  
Release Profile ◽  
Drug Release Profile ◽  
H Nmr ◽  
Ft Ir ◽  
Potential Antitumor

A series of polyesters containing 5-fluorouracil in the main chain were prepared by reacting potassium salt of 5-fluorouracil with different molecular weight ω-chloroalkyl chloroacetyl esters.The copolymers were characterized by FT-IR, 1H-NMR, VPO and UV spectroscopy. The drug release profile in vitro of the copolymers were studied, the results showed prodrug could slow release 5-FU or 5-FU units in different solution, they may be likely to become potential antitumor prodrug.

Characterization of the phenolic constituents in Mauritian endemic plants as determinants of their antioxidant activities in vitro

2006 ◽  
Vol 163 (8) ◽  
pp. 787-799 ◽  
Author(s):  
Vidushi S. Neergheen ◽  
Muhammad A. Soobrattee ◽  
Theeshan Bahorun ◽  
Okezie I. Aruoma
Keyword(s):  
Antioxidant Activities ◽  
Endemic Plants ◽  
Phenolic Constituents

scholarly journals Synthesis and Characterization of New Amino Acid-Schiff Bases and Studies their Effects on the Activity of ACP, PAP and NPA Enzymes (In Vitro)

2012 ◽  
Vol 9 (2) ◽  
pp. 962-969 ◽  
Author(s):  
Zahraa Salim M. Al-Garawi ◽  
Ivan Hameed R. Tomi ◽  
Ali Hussein R. Al-Daraji
Keyword(s):  
Schiff Base ◽  
Condensation Reaction ◽  
Synthesis And Characterization ◽  
Activation Effect ◽  
Inhibition Effect ◽  
H Nmr ◽  
Ft Ir ◽  
High Concentrations

In this study, two new Schiff base compounds derived from the condensation reaction ofL-glycine andL-tryptophan with 4-methylbenzal-dehyde have been synthesized. The Schiff base compounds were characterized by FT-IR, UV and1H NMR spectroscopy. Their effects on the activity of total (ACP), prostatic (PAP) and non prostatic (NPA) acid phosphatase enzymes were studied. The Schiff base derived fromL-glycine (A) demonstrated inhibition effect on the ACP and NPA activities and activation effect on PAP activity. The Schiff base derived fromL-tryptophan (B) demonstrated semi fixed inhibition effects on the ACP and NPA activities at high concentrations (5.5×10-2, 5.5×10-3and 5.5×10-4M) and activator effect at low concentration (5.5×10-5M) while it was exhibits as activator on PAP activity.

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