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bijps-874
Synthesis, Characterization and Preliminary Anticancer Study of Novel 5-fluorouracil Conjugate with Pyrrolidine Dithiocarbamate as a Mutual Anticancer Prodrug
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 5-Fluorouracil is one of the commonly used chemotherapy drugs in anticancer therapy; unfortunately treatment with 5-FU by solely has many drawbacks  low lipophilicity, low permeability, low molecular weight, and its relatively poor plasma protein binding; also a brief half-life therefore frequent administration is required to maintain the optimal therapeutic plasma level which in addition to its poor selectivity, drug resistance and limited penetration to cancer cells; leads to increased incidence of side-effects to healthy cells/tissues and low response rates. In order to minimize these drawbacks; 5-FU was chemically  conjugated with pyrrolidine dithiocarbamate (PDTC) in a mutual prodrug moiety (S-(9H-purin-6-yl) 3-((pyrrolidine-1-carbonothioyl)thio)propanethioate) "compound [IV]" with (chloroacetic acid) and (chloroethanol) being the linkers ;synthesized prodrug and intermediates were characterized and identified using FTIR ,1H NMR and all the results shown good agreements with the proposed chemical structures of the synthesized compounds.  ; in-vitro preliminary cytotoxicity study was conducted for compound [IV] and 5-FU on CAL 51 and B16V cell lines ,results showed  enhanced cytotoxic effects for [IV] over 5-FU.

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Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
synthesis and characterization
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chloride or poluacrulic acid with different primary amines to mesuring==================================638one hundred three patinents with rheumatic symptoms were include in this study and their sera tested for

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Publication Date
Wed Apr 26 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Antibactrial Study of New 2-Amino-5-Aryl- 1,3-Thiazole-4-Carboxylic Acid Derivatives
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2-Amino-5-aryl- 1,3-thiazole-4-carboxylic acid (A1-A3) were synthesized from the reaction of various aromatic aldehyde with dichloro acetic acid and thiourea. The synthesis of 2-[[(Saminosulfinim-idoyl)(aryl)methyl](benzoyl)amino]-5-aryl-1,3-thiazole-4-carboxylic acid (A22-A30) was perfomed starting from (A1-A3) by two steps using Schiff's base (A4-A12) prepared  from the reactant compounds (A1-A3) with different aromatic aldehyde. Finally two types of imide derivatives were obtained from reactant compounds (A1-A3) with malic anhydride (A31-A33) and phthalic anhydride (A34-A36) in the presence of glacial acetic acid. All proposed structures were supported by FT-IR and UV-Visible spectroscopic data.  
 

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Publication Date
Tue Aug 04 2020
Journal Name
Indonesian Journal Of Pharmacy
Design and Synthesis of Novel Derivatives of 4-(6-(4-Substituted Phenyl)-7H-[1,2,4] Triazolo[3,4-b][1,3,4]Thiadiazin-3- yl) Phenol as a Potent Inhibitor of Tubulin with Antitumor Activity
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Publication Date
Sun Oct 01 2023
Journal Name
Baghdad Science Journal
Ghrelin and Obestatin Levels as a Novel Marker in Iraqi Obese Children
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Obesity is an escalating health problem in developing countries. One to ten children worldwide are overweight in a report showed by the International Obesity Task Force. Ghrelin, orexigenic peptide, has 28 amino acids, it is considered the greatest remarkable promotion in the last two decades for understanding the physiological changes of action regu­lating food intake and hunger. Obestatin is a 23-amino acid peptide nearly connected to ghrelin that secures from substitutio

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Publication Date
Tue Oct 01 2024
Journal Name
Results In Chemistry
Microwave synthesis, density functional theory study and antiproliferative activity of the novel spiropyrazole derivatives
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Publication Date
Thu Apr 25 2019
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
SYNTHESIS, CHARACTERIZATION AND STUDY THE ANTIBACTERIAL ACTIVITY OF SOME DISUBSTUTITED-1,3,4-OXADIAZOLE DERIVATIVES: SYNTHESIS, CHARACTERIZATION AND STUDY THE ANTIBACTERIAL ACTIVITY OF SOME DISUBSTUTITED-1,3,4-OXADIAZOLE DERIVATIVES
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The purpose of this study is to determine the useful of Schiff bases derivatives containing (oxazepine, tetrazole) rings with biological activity which can be used as drug and antimicrobial, the present work is started from [Binary (2,5(4,'4-diaminophenyl) – 1,3,4 – oxadiazole]. A variety of Schiff bases and heterocyclic (oxazepine, tetrazole) have been synthesis, and confirm that structures by physical properties , FTIR , 1H-NMR, 13C-NMR, elemental analysis, [Microbial study against three type of bacteria (staphylococcus aurea and klebsiella pneumonia) and (Canadida albncans) fungi].All analyzation performed in center of consulatation University of Jordan.

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Publication Date
Thu Dec 28 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis, Characterization and Antibacterial Activity of New Chalcones Derived from New Aldehyde; 4-[5-(4`tolyl)-1,3,4-thiadiazole-2-yl] benzaldehyde
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 New chalcones of  -{ -  -   -   y  -     - hi di z  e- -y    he y  - -    e e- -  e-    -        - substituted phenyl have been prepared from condensation of  a new of  4-[5-(4`-tolyl)1,3,4-thiadiazole-2-yl] benzaldehyde (which is synthesized by the reaction of  2- amino-5- (4`-tolyl) -1,3,4-thiadiazole and benzaldehyde) with 3- or 4- substituted acetophenones in alkaline medium. The physical, CHNS analysis and spectral data of the synthesized compounds were determined. The biological activity evaluated of new compounds showed that many of these compounds possess antiba

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Publication Date
Wed Apr 12 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of Novel 1,3-Oxazepines Derived from Diamic Acid : N,N‾-Bis-(4-methyl phenyl ) pyromellitamic Diacid
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    The symmetrical N,N‾-Bis-(4-methyl phenyl) pyromellitamic diacid  (I) was synthesized from the reaction of toludine with pyromellitic dianhydride in dry acetone. Esterification of amic acid (I) with dimethyl sulphate in basic medium using acetone as a solvent give symmetrical N,N‾-bis-( 4- methyl phenyl ) pyromellitam diacetate (II).  The condensation of new ester with hydrazine hydrate in ethanol  leads to the formation symmetrical N,N‾-bis- (4-methyl phenyl) pyromellitamic hydrazide (III). New symmetrical 1,3-oxazepine derivatives (V)a-e  can be synthesized  from the reaction of the new synthesized Schiff bases (III)a-e (which are synthesized from the reaction new hydrazide

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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis and Characterization of Some New Monemer and Polymers Containing Hetero Cyclic Rings With Study of Their Physical Properties.
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Number of new polyester and polyamide are prepared as derivatives from 5,5`-(1,4-phenylene)-bis-(1,3,4-thiadiazole-2-amine) [C1], three series of heterocyclic compounds were synthesized.The first series includes the Schiff base [C2] prepared from the reaction between compound [C1] with p-hydroxy benzaldehyde in presence of acetic acid and absolute ethanol , then these derivatives have reaction with maleic anhydride , phthalic anhydride and sodium azide, respectively to obtain the compounds [C3-5] contaning (oxazepine and tetrazole) rings.The third series of compounds [C1-5] has transformed to their polymers [C6-15] by reaction with adipoyl chloride and glutroyl chloride , respectively. The reaction was followed by T.L.C and ident

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Publication Date
Fri Feb 10 2012
Journal Name
Molecules
Design, Synthesis and Preliminary Pharmacological Evaluation of New Non-Steroidal Anti-Inflammatory Agents Having a 4-(Methylsulfonyl) Aniline Pharmacophore
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A series of 4-(methylsulfonyl)aniline derivatives were synthesized in order to obtain new compounds as a potential anti-inflammatory agents with expected selectivity against COX-2 enzyme. In vivo acute anti-inflammatory activity of the final compounds 11–14 was evaluated in rat using an egg-white induced edema model of inflammation in a dose equivalent to 3 mg/Kg of diclofenac sodium. All tested compounds produced significant reduction of paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the activity of compounds 11 and 14 was significantly higher than that of diclofenac sodium (at 3 mg/Kg) in the 120–300 minute time interval, while compound 12 expressed a comparable effect to that of di

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