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bijps-413
Synthesis of new Conjugates of some NSAIDs with Sulfonamide as Possible Mutual Prodrugs using Tyrosine Spacer for Colon Targeted Drug Delivery
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The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of  inflammation and infections in colon).

Key words: Mutual prodrug, Ester linkage, Azo bond, Colon targeting

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Publication Date
Wed May 16 2018
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Study the Mesomorphic Behaviour of New N- acetyl and Their Diazetine: Mono and Twin
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   Synthesis ,characterization of new mono and twin  compounds containing heterocyclic four member ring as, 1,3- diazetine by four steps. The first step; includes  preparation of 2- amino thiazole derivatives [I]a-c via ring closure reaction between acetophenone derivatives   with thiourea in I2,  while the second step includes condensation reaction between 2-amino thaizole derivatives[I]a-c and  p-methoxy benzaldehyde to produce Schiff bases[II]a-c. The third step includes neculophilic attach from imine group toacetyl chloride to give N- acetyl cross bonding[III]a-c.Finally ; the  fourth step is completed by the reaction of N- acetyl deri

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Publication Date
Wed Jun 26 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Acute Anti-inflammatory Evaluation of New Mefenamic Acid Derivatives Having 4-Thiazolidinone Nucleus
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Mefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug's potential side effects, new series of 4-t

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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
Sat Nov 04 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Preliminary Anti-Inflammatory and Anti-Microbial Evaluation of New 4,5-Dihydro-1H-Pyrazole Derivatives
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Abstract      Organic compounds with pyrazole cores have a variety of uses, notably in the pharmaceutical and agrochemical sectors. The interest in creating pyrazole compounds, examining their many features, and looking for potential uses is growing. Our work has concert with synthesis of  chalcones and pyrazolines, then finally pyrazoline-aniline derivatives and evaluation their anti-inflammatory, antibacterial and antifungal activities

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Publication Date
Thu Feb 01 2018
Journal Name
Journal Of Pharmacy Research
Synthesis and antimicrobial evaluation of new-[2-amino-4- (4-chloro-/4-bromophenyl)-1,3-thiazole derivatives
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Publication Date
Thu Oct 31 2019
Journal Name
Asian Journal Of Pharmaceutical And Clinical Research
DESIGN, SYNTHESIS, DOCKING, ANTITUMOR SCREENING, AND ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION PREDICTION OF NEW HESPERDIN DERIVATIVE
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Objective: Hesperidin (HSP) is a pharmacologically active organic compound found in citrus fruits and peppermint. We synthesized a new HSP derivative by reacting it with 5-Amino-1,3,4-thiadiazole-2-thiol in acetic acid. Methods: This compound was characterized by Fourier-transform infrared, proton nuclear magnetic resonance, and electron impact mass spectra. A molecular docking study explores the predicted binding of the compound and its possible mode of action. Bioavailability, site of absorption, drug mimic, and topological polar surface was predicted using absorption, distribution, metabolism, and excretion (ADME) studies. Results: The docking study predicts that the new compound binds to the active sites of Aurora-B

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Publication Date
Mon May 15 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis of New Schiff Bases and 2,3-Disubstituted 1,3-Thiazolidin-4-one Derivatives Containing Benzothiazole Moiety
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  Two series of Schiff Bases and 2,3-disubstituted-1,3-thiazolidin-4-one derivatives  were synthesized . Reaction of 2-mercaptobenzothiazole with α-chloro acetic acid gave compound[I]. Esterification of carboxylic moity of compound [I] , using absolute methanol in the presence of conc . H2SO4 yielded acorresebonding ester  [II] , wich was condensation with hydrazine hydrate to give acid hydrazide [III] . The new Schiff bases [V]n were synthesized by reaction of acid hydrizide with dialdehyde [IV]n  in the presence of glacial acetic acid . The thiazolidinone derivatives [VI]n  have been obtained from the azomethines through the addition of thioglycolic acid . Their chemical structures have been confirmed by mel

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Publication Date
Wed Mar 25 2020
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization and Antimicrobial Evaluation of New Azo Compounds Derived from Sulfonamides and Isatin Schiff Base
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The present study deals with the synthesis of four different azo-azomethine derivatives; this is done by two steps; the first step is diazotization of sulfonamides (sulfanilamide, sulfacetamide, sulfamethoxazole, and sulfadiazine) separately, followed by the second step; the coupling reaction of diazotized compounds with isatin bis-Schiff base named 3-((4-nitrobenzylidene) hydrazono)indolin-2-one. The later one (bis-Schiff base) was synthesized by the reaction of 3-hydrazono-indolin-2-one with p-nitrobenzaldehyde. The chemical structures of newly synthesized compounds were approved on the basis of their FTIR, 1H-NMR, and CHNS elemental analysis data results. The synthesized azo compounds were tested in vitro for their antimicrobial potentia

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Publication Date
Mon Jan 31 2022
Journal Name
Iraqi Journal Of Science
Synthesis and Characterization of Several New Copolymers Based on Maleimides Bearing 1, 3, 4-Oxadiazole Moiety
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A series of new copolyimides containing pendant 1,3,4-oxadiazole moiety were synthesized via multisteps. In the first step five N-(5-substituted-1,3,4-oxadiazole-2-yl)maleamic acids were prepared via reaction of maleic anhydride with 2-amino-5-substituted-1,3,4-oxadiazoles. The obtained amic acids were dehydrated in the second step affording the corresponding N-(5-substituted-1,3,4-oxadiazole-2-yl) maleimides. In the third step the newly synthesized maleimides were introduced successfully in free radical copolymerization reaction with four vinylic monomers including acrylo nitrile, methacrylonitrile, methyl acrylate and methyl meth acrylate respectively producing twelve new copolymers having different physical properties which may serve

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Publication Date
Sat Dec 01 2018
Journal Name
Applied Soft Computing
A new evolutionary algorithm with locally assisted heuristic for complex detection in protein interaction networks
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