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

2011 ◽  
Vol 284-286 ◽  
pp. 1728-1731
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 polyesteramide containing 5-fluorouracil in the main chain were prepared by reacting potassium salt of 5-fluorouracil with N-(2-chloroacetoxylalkyl)-chloroacetamide.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.

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.

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 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.

Preparation and Interaction of Modified PHS and CMC Liquid Composites

2014 ◽  
Vol 1035 ◽  
pp. 204-211 ◽  
Author(s):  
Xiao Ling Xu ◽  
Min Zhang ◽  
Ji Qing Song ◽  
Wen Qing He
Keyword(s):  
Molecular Dynamics ◽  
Polyethylene Glycol ◽  
Main Chain ◽  
Composite Films ◽  
Interfacial Interaction ◽  
Structure Characterization ◽  
Nmr Spectrum ◽  
H Nmr ◽  
Ft Ir

Novel liquid composites were successfully prepared by blending copolymer (PEG/PHS) and carboxymethyl cellulose (CMC) in this work. PEG/PHS was achieved by introducing polyethylene glycol (PEG) into the main chain of poly hexanediol succinic (PHS). The results showed that the structure characterization of PEG/PHS was displayed in 1H NMR spectrum. The interaction existed between PEG/PHS and CMC which was validated in FT-IR and SEM. This conjecture was simulated by molecular dynamics under the software YASARA. Because of the existence of interfacial interaction, composites films kept good thermal performance and the flexibility of composite films was greatly improved.

Synthesis and Characterization of 5-Fluorouracil and Polyethylene Glycol Esters as Prodrugs

2011 ◽  
Vol 287-290 ◽  
pp. 1509-1512 ◽  
Author(s):  
Cheng Wu Li ◽  
Gang Li ◽  
Ji Cheng Zuo
Keyword(s):  
Molecular Weight ◽  
Polyethylene Glycol ◽  
Water Solubility ◽  
Uv Spectroscopy ◽  
Chloroacetic Acid ◽  
Synthesis And Characterization ◽  
Drug Release Rate ◽  
H Nmr ◽  
Ft Ir

A series of novel polyethylene glycol derivates was synthesized by esterification of chloroacetic acid with polyethylene glycol.The PEG-5-FU conjugates were characterized by FT-IR,1H-NMR and UV spectroscopy. The result showed that 5-FU was successfully connected to the ends of PEG ester. Drug content of PEG2000-5-FU conjugate achieved 17.4%. As the molecular weight of PEG increased, the water solubility of prodrugs improved. When the molecular weight of PEG reached 2000, the conjugate had the best water solubility and the highest drug release rate.

scholarly journals Formulation of Quaternized Aminated Chitosan Nanoparticles for Efficient Encapsulation and Slow Release of Curcumin

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 449
Author(s):  
Ahmed M. Omer ◽  
Zyta M. Ziora ◽  
Tamer M. Tamer ◽  
Randa E. Khalifa ◽  
Mohamed A. Hassan ◽  
...  
Keyword(s):  
Slow Release ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
Gastric Fluid ◽  
Release Profile ◽  
Simulated Gastric Fluid ◽  
Maximum Value ◽  
Structure Surface ◽  
Drug Encapsulation Efficiency

An effective drug nanocarrier was developed on the basis of a quaternized aminated chitosan (Q-AmCs) derivative for the efficient encapsulation and slow release of the curcumin (Cur)-drug. A simple ionic gelation method was conducted to formulate Q-AmCs nanoparticles (NPs), using different ratios of sodium tripolyphosphate (TPP) as an ionic crosslinker. Various characterization tools were employed to investigate the structure, surface morphology, and thermal properties of the formulated nanoparticles. The formulated Q-AmCs NPs displayed a smaller particle size of 162 ± 9.10 nm, and higher surface positive charges, with a maximum potential of +48.3 mV, compared to native aminated chitosan (AmCs) NPs (231 ± 7.14 nm, +32.8 mV). The Cur-drug encapsulation efficiency was greatly improved and reached a maximum value of 94.4 ± 0.91%, compared to 75.0 ± 1.13% for AmCs NPs. Moreover, the in vitro Cur-release profile was investigated under the conditions of simulated gastric fluid [SGF; pH 1.2] and simulated colon fluid [SCF; pH 7.4]. For Q-AmCs NPs, the Cur-release rate was meaningfully decreased, and recorded a cumulative release value of 54.0% at pH 7.4, compared to 73.0% for AmCs NPs. The formulated nanoparticles exhibited acceptable biocompatibility and biodegradability. These findings emphasize that Q-AmCs NPs have an outstanding potential for the delivery and slow release of anticancer drugs.

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 of Eco-friendly Nano-Structured Biosurfactants from Vegetable Oil Sources and Characterization of Their Interfacial Properties for Cosmetic Applications

MRS Advances ◽  
2018 ◽  
Vol 4 (07) ◽  
pp. 377-384 ◽  
Author(s):  
DaNan Yea ◽  
SeonHui Jo ◽  
JongChoo Lim
Keyword(s):  
Raw Materials ◽  
Coconut Oil ◽  
Interfacial Properties ◽  
Interfacial Property ◽  
Solution Stability ◽  
H Nmr ◽  
Wetting Property ◽  
Potential Applicability ◽  
Ft Ir

ABSTRACTIn this study, 3 types of zwitterionic phospholipid biosurfactants LDP(S), CDP(S) and CTDP(S) were prepared from 3 different raw materials such as rapeseed oil, coconut oil and cottonseed oil respectively. The structure of the resulting phospholipid biosurfactants was elucidated by FT-IR, 1H NMR and 13C NMR spectroscopies and their interfacial properties have been examined such as CMC, static surface tension, wetting property, solution stability, and foam property. Interfacial property measurement and prescription test in cosmetic formulation prepared with the newly synthesized biosurfactants revealed that CDP(S) biosurfactant possesses excellent mildness and superior interfacial properties, indicating the potential applicability in cosmetic product formulations.

scholarly journals SYNTHESIS AND STRUCTURAL ELUCIDATION OF AMINO ACETYLENIC AND THIOCARBAMATES DERIVATIVES FOR 2-MERCAPTOBENZOTHIAZOLE AS ANTIMICROBIAL AGENTS

2017 ◽  
Vol 9 (2) ◽  
pp. 192
Author(s):  
Aseel Alsarahni ◽  
Zuhair Muhi Eldeen ◽  
Elham Al-kaissi ◽  
Ibrahim Al- Adham ◽  
Najah Al-muhtaseb
Keyword(s):  
Antimicrobial Activity ◽  
Elemental Analysis ◽  
Antimicrobial Agents ◽  
Diffusion Method ◽  
Benzothiazole Derivatives ◽  
H Nmr ◽  
Ft Ir ◽  
Potential Antimicrobial Activity ◽  
C Nmr

<p><strong>Objective: </strong>To design and synthesize amino acetylenic and thiocarbonate of 2-mercapto-1,3-benthiazoles as potential antimicrobial agents.</p><p><strong>Methods: </strong>A new series of 2-{[4-(t-amino-1-yl) but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole derivatives (AZ1-AZ6), and S-1,3-benzothiazol-2-yl-O-alkyl carbonothioate derivatives were synthesised, with the aim that the target compounds show new and potential antimicrobial activity. The elemental analysis was indicated by the EuroEA elemental analyzer, and biological characterization was via IR, <sup>1</sup>H-NMR, [13]C-NMR, DSC were determined with the aid of Bruker FT-IR and Varian 300 MHz spectrometer using DMSO-d<sub>6</sub> as a solvent.<em> </em><em>In vitro </em>antimicrobial activity, evaluation was done for the synthesised compounds, by agar diffusion method and broth dilution test. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) were determined. <em></em></p><p><strong>Results: </strong>The IR, <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, DSC and elemental analysis were consistent with the assigned structures. Compound of 2-{[4-(4-methylpiperazin-1-yl)but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole (AZ1), 2-{[4-(2-methylpiperidin-1-yl)but-2-yn-1-yl]sulfanyl}-1,3-benzothiazole (AZ2), 2-{[4-(piperidin-1-yl) but-2-yn-1-yl]sulfanyl}-1, 3-benzothiazole (AZ6), S-1,3-benzothiazol-2-yl-O-ethyl carbonothioate (AZ7), and S-1,3-benzothiazol-2-yl-O-(2-methylpropyl) carbonothioate (AZ9) showed the highest antimicrobial activity against <em>Pseudomonas aeruginosa </em>(<em>P. aeruginosa</em>), AZ-9 demonstrated the highest antifungal activity against <em>Candida albicans </em>(<em>C. albicans</em>), with MIC of 31.25 µg/ml.</p><p><strong>Conclusion: </strong>These promising results promoted our interest to investigate other structural analogues for their antimicrobial activity further.</p>

Electrochemically Synthesis and Characterization of Copolymers Based on 1, 4-Diethoxybenzene and 3, 4-Ethylenedioxythiophene

2011 ◽  
Vol 335-336 ◽  
pp. 989-993
Author(s):  
Mi Ouyang ◽  
Zhen Wei Yu ◽  
Yi Xu ◽  
Yu Jian Zhang ◽  
Cheng Zhang
Keyword(s):  
Cyclic Voltammetry ◽  
Ir Spectroscopy ◽  
Feed Ratio ◽  
Synthesis And Characterization ◽  
Monomer Mixture ◽  
Long Wavelength ◽  
H Nmr ◽  
Ft Ir ◽  
Ft Ir Spectroscopy

Copolymers based on 1, 4-diethoxybenzene (DEB) and 3, 4-ethylenedioxythiophene (EDOT) were electrochemically synthesized and characterized. The structures of the copolymers were established by 1H NMR and FT-IR spectroscopy. The results indicated the final product was a copolymer instead of a blend or a composite. The physical properties were systematically investigated by cyclic voltammetry, UV-vis absorption and fluorescence. The PL maximum of copolymers presented obviously red-shift to long wavelength as the feed ratio of EDOT in monomer mixture increased.

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