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Design, synthesis, insilco study and biological evaluation of new isatin-sulfonamide derivatives by using mono amide linker as possible as histone deacetylase inhibitors
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Aim: To evaluate the cytotoxic activity of newly synthesized a series of novel HDAC inhibitors comprising sulfonamide as zinc binding group and Isatin derivatives as cap group joined by mono amide linker as required to act as HDAC inhibitors. Materials and Methods: The utilization of sulfonamide as zinc binding group joined by N-alkylation reaction with ethyl-bromo hexanoate as linker group that joined by amide reaction with Isatin derivatives as cap groups which known to possess antitumor activity in the designed of new histone deacetylase inhibitors and using the docking and MTT assay to evaluate the compounds. Results: Four compounds have been synthesized and characterized successfully by ART-FTIR, NMR and ESI-Ms. the compounds were synthesized and characterized by successfully by ART-FTIR, NMR and ESI- Ms. Assessed for their cytotoxic activity against human colon adenocarcinoma MCF-7 (IC50, I=105.15, II=60.00, III=54.11, IV=56.57, vorinostat=28.41) and hepatoblastoma HepG2 (IC50, I=63.91, II=135.18, III=118.85, IV=51.46, vorinostat=37.50). Most of them exhibited potent HDAC inhibitory activity and significant cytotoxicity. Conclusions: The synthesized compounds (I, II, III and IV) showed cytotoxicity toward MCF-7 and HepG2 cancer cell lines and their docking analysis provided a preliminary indication that they are viable [HDAC6] candidates.

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Publication Date
Sun Dec 22 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and In-Vitro Evaluation of Darifenacin Hydrobromide as Buccal Films
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         Darifenacin hydrobromide (DH) is the more recent uroselective M3 receptor antagonist for treating uncomplicated overactive bladder (OAB). This study was aimed to formulate DH as fast dissolving buccal films (FDBFs) using a solvent casting method to enhance patient’s compliance.

         Films were prepared by using polyvinyl alcohol (PVA) as a film forming polymer. Different types and concentrations of superdisintegrants (croscarmellose sodium, sodium starch glycolate, indion 414) were used to select the best formula by studying the physicochemical properties of the films, disintegration time (DT) and percent drug release.

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Publication Date
Wed Aug 18 2010
Journal Name
Journal Of Kerbala University
Synthesis of New Type of Sugar Ligands Starting from D-Glucose And Screening Their Biological Activity
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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
Preparation and Evaluation of PolyVinyl Alcohol Derivative as Antimicrobial and Antifungal Agents
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Polyvinal alcohol was Cynoethylated , complex compound with Iodin in presence of Cu++ ions were preparated and their ultra violet (U.V) and infra red( IR) spectra were investigated. The prepared derivative and complexes were evaluated as antibacterial and antifungal agents following the standard dilution method. MIC(minimum inhibitory concentration) for each polymer using ten types of gram + ve and gram _ ve bacteria were determinated in addition to three types of fungi. The results obtainded showed that MIC, s were around 0.0011 × 103 molar for different polymetric derivatives tried.

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Publication Date
Tue Mar 30 2021
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Biological Activity Evaluation of Some Pyrazoles, Thiazoles and Oxazoles Derived from 2-Mercaptoaniline
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    Synthesis of 2-mercaptobenzothiazole (A1) is performed from the reaction of  o-aminothiophenol and carbon disulfide CS2 in ethanol under basic condition. Compound (A1)  is reacted with chloro acetyl chloride to give compound (A2). Hydrazide acid compound (A3) is obtained from the reaction of compound (A2) with  hydrazine hydrate in ethanol under reflux in the presence of glacial acetic acid .The reaction of hydrazide acid compound (A3) with ethyl acetoacetate gives pyrazole compound (A4). The new hydrazone  compound (A5) was prepared from the reaction of compound (A3) with  benzaldehyde. Reaction of compound

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Publication Date
Fri Apr 01 2022
Journal Name
Chemical Methodologies
Design, Synthesis of Imidazolone and Oxazepine Derivatives Bearing Imidazo (2, 1-b) Thiazole along with its Antimicrobial Activity
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A new methodology was applied to the synthesis of new imidazolones and oxyazepine derivatives containing imidazo thiazole fused rings. Starting with 5-(4-bromo phenyl) imidazo (2, 1-b) thiazole, which was synthesized using the standard procedure, the Carbaldehyed group was introduced at position 6 of 5-(4-bromo phenyl) imidazo (2, 1-b) thiazole. Then, this 6-carbaldehyed derivative was condensed with different substituted aromatic amines to afford new Schiff bases. The latter were cyclized into new oxazepine and imidazolone derivatives by using phthalic anhydride and glycine, respectively. These new derivatives were characterized by using FT-IR, 1HHNMR, and 13CNMR spectra, as well as examined (evaluated) for anti-bacterial and anti-fungal a

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Publication Date
Wed May 01 2024
Journal Name
Baghdad Science Journal
Synthesis, Spectroscopy and Biological Activity Study of Some New Complexes with Schiff Base Derived From Malonic Acid Dihydrazide with 2-pyridine Crboxaldehyde
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تم تحضير ثلاث معقدات جديدة Ni (II)و Cu (II) و Zn (II) باستخدام الليكند المحضر الجديد من تفاعل حامض مالونيك ثنائي هيدرازايد مع 2-بيريدين كربوكسالديهايد. حيث شخصت المعقدات لمحضرة وكذلك الليكند باستخدام تقنيات مختلفة مثل FT-IR و UV-Vis و Mass و 1H-NMR و 13C-NMR وتحليل العناصر CHN و تقدير محتوى  الكلور والموصلية المولارية والحساسية المغناطيسية والامتصاص الذري لتشخيص هذه المركبات. لكل معقد محضر جديد من النيكل والنحاس والزنك ، كشفت نتائج ا

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Publication Date
Wed Nov 24 2021
Journal Name
International Journal Of Drug Delivery Technology
Comparison among the Synthesis of Some Azomethine Derivatives by Classical and Non-classical Methods
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الوصف In this time, most researchers toward about preparation of compounds according to green chemistry. This research describes the preparation of 2-fluoro-5-(substituted benzylideneamino) benzonitrile under reflux and microwave methods. Six azomethine compounds (B1-6) were synthesized by two methods under reflux and assisted microwave with the comparison between the two methods. Reflux method was prepared of azomethine (B1-6) by reaction of 5-amino-2-fluorobenzonitrile with some aldehyde derivatives with (50–100) mL of absolute ethanol and some quantity of GAA and time is limited between (2–5) hours with a yield between (60–70) percent with recrystallization for appropriate solvents. But the microwave-assisted method was synthe

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Publication Date
Fri Jun 25 2021
Journal Name
International Journal Of Drug Delivery Technology
Comparison among the Synthesis of Some Azomethine Derivatives by Classical and Non-classical Methods
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In this time, most researchers toward about preparation of compounds according to green chemistry. This research describes the preparation of 2-fluoro-5-(substituted benzylideneamino) benzonitrile under reflux and microwave methods. Six azomethine compounds (B1-6) were synthesized by two methods under reflux and assisted microwave with the comparison between the two methods. Reflux method was prepared of azomethine (B1-6) by reaction of 5-amino-2-fluorobenzonitrile with some aldehyde derivatives with (50–100) mL of absolute ethanol and some quantity of GAA and time is limited between (2–5) hours with a yield between (60–70) percent with recrystallization for appropriate solvents. But the microwave-assisted method was synthesized of co

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Publication Date
Thu Jun 30 2022
Journal Name
International Journal Of Drug Delivery Technology
Comparison among the Synthesis of Some Azomethine Derivatives by Classical and Non-classical Methods
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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Spectroscopic Study for Determination of Amoxicillin Using Cobalt(II) as Complexing Metal
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         This study includes analytical methods for the determination of the drug amoxicillin trihydrate (Amox.) in some pharmaceutical preparations using Cobalt ion (Co(II)) as complexing metal. The best conditions for complexation were: the reaction time was 20 minutes, pH=1.5 and the best temperature of reaction was 70 ËšC. Benzyl alcohol was the best solvent for extraction the complex.

Keywords: Amoxicillin, Cobalt(II), Complex, Molar ratio.

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