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SYNTHESIS OF NEW PROPRANOLOL DERIVATIVES AS POSSIBLE PRODRUGS
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Propranolol is a nonselective-adrenergic blocker used in the treatment of hypertension, cardiac arrhythmias, and angina pectoris. A significant problem in propranolol therapy is that it undergoes extensive presystemic metabolism after oral administration leading to reduced bioavailability. In this study, two new propranolol derivatives have been designed, synthesized and characterized. These compounds were formed by acylation of propranolol followed by nucleophilic substitution reaction of acylated propranolol, these derivatives were analyzed for IR, CHN, melting points, and evaluated for their lipophilic properties compared with propranolol. The lower partition coefficient of these two derivatives revealed that the prodrug approach may be an effective means of avoiding first- pass metabolism.

Publication Date
Wed Nov 24 2021
Journal Name
Iraqi Journal Of Science
Synthesis and Biological Activity Evaluation of New Sulfonamid Derivatives
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New sulfonamide derivatives comprising azide, 1, 2, 3- triazole, azo , chalcone and Schiff base moieties had synthesized. The structures of the new compunds have been confirmed byFT-IR and ¹H-NMR spectra. The synthesized derivatives have been screened for antimicrobial and in vitro antioxidant properties. The results of this investigation revealed that the newly synthesized compounds have good antimicrobialand antioxidant activities.

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Publication Date
Fri May 01 2009
Journal Name
Diyala Journal For Pure Science
Synthesis of Schiff bases of 2-thio-5-aryl-1,3,4- oxadiazole derivatives of possible biological activity
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In this study, new derivatives of Schiff bases of 2-thio-5-aryl1,3,4-oxadiazole have been synthesized. The structures of these derivatives were characterized from their melting points, infrared spectroscopy and elemental analysis. The Schiff bases derivatives were tested for inhibition of E-coli and were all found to be active.

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Publication Date
Fri Mar 01 2024
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New 2-amino-5-chlorobenzothiazole Derivatives Containing Different Types of Heterocyclic as Antifungal Activity
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Nine new compounds of 2-amino-5-chlorobenzothiazole derivatives were synthesized. These new compounds were formed through the reaction of 2-amino-5-chlorobenzothiazole 1 with ethyl chloroacetate and KOH, which gave an ester derivative 2, followed by refluxing compound 2 with hydrazine hydrate to afford hydrazide derivative 3. The reaction of compound 3 with CS2 and KOH gave 1,3,4-oxadiazole-2-thiol derivative 4, and then the reaction of compound 2 with thiosemicarbazide to produce compound 5  then treated it with 4%NaOH led to ring closure to provide 1,2,4-triazole-3-thiol derivative

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Scopus Crossref
Publication Date
Sun Jun 02 2013
Journal Name
Baghdad Science Journal
Synthesis and Characterizationof Some New Phenolic Schiff Bases Derivatives
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Starting from bis (4,4'-diamino phenoxy) ethan(1), a variety of phenolicschiff bases (methylolic, etheric, epoxy) derivatives have been synthesized. All proposed structure were supported by FTIR, 1H-NMR, 13C-NMR Elemental analysis, some derivatives evaluated by thermal analysis (TGA).

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Crossref
Publication Date
Mon Jun 03 2019
Journal Name
Journal Of Global Pharma Technology
New Diquinazoline Derivatives: Synthesis and Evaluation of AntiBacterial Activi
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Oxazine and quinazoline has a very important in organic chemistry especially in hetero cyclic fields. this research consist the preparation of 4H,4'H-2,2'-bibenzo[d][1,3]oxazine-4,4'-dione compound (1) from di acid chloride with 2-aminobenzoic acid in pyridine as solvent to give compound (2) 3,3'-diamino-2,2'- biquinazoline-4,4'(3H,3'H)-dione .compound 2 include free amino group .this compound was reacted with maleic and phthalic anhydride for synthesized of cyclic imide compounds (3,4).another reaction for compound 2 with some substituted aromatic aldehyde for prepared of some novel Schiff bases (5-9) contains quinazoline ring. compound 1 was treated with sulfathiazole and sulfadiazine for synthesized of sulfa compounds contains sulf

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Publication Date
Sun Mar 12 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of Some New Hydrazides and Their Derivatives
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New hydrazide compounds (A2) and (A9) were prepared from their corresponding esters (A1, A8) .These esters were also prepared from their precursors 5-ethoxy carbonyl-(4methoxyphenyl)-6-methyl-1,2,3,4-tetrahydropyrimidine-2-thione (A1) via multicomponent reaction type and from hippuric acid respectively. The hydrazide compounds were then allowed to react with some aldehydes forming the corresponding hydrazones (A3-7) and (A1014). The synthesized compounds were characterized by IR, 1H-NMR, 13C-NMR, and Mass spectroscopies and well discussed. .

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Publication Date
Sun Apr 23 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and antimicrobial evaluation of new 1,3,4 – Thiadiazole Derivatives
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The amino thiadiazole [I] on treatment with aromatic aldehydes yielded Schiff bases [IIa-c] , which cyclized to thiazolidinone [IIIa-c] derivatives by reaction with thioglycolic acid .Reaction of carbon disulfide and methyl iodide with [I] gavedithiomethyl[IV] which on treatment with o-phenylenediamine gave the condensed N-Imidazolythiadiazolylamine [V] , However , reaction of [I] with phenylisocyanate and phenylisothiocyanate afforded the carbamideand carbothiamide derivatives[VI.VII]a-c. The structure of these compounds was characterized from their  melting point , FTIR spectroscopy and elementalanalysis

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Publication Date
Sat Jun 03 2023
Journal Name
Iraqi Journal Of Science
Synthesis and Characterization of Some New Derivatives From 2-Mercaptobenzoxazole
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In this work 2-mercaptobenzoxazole (2-MBO) (1), was prepared by using homemade Auto clave .The synthesis involve treatment of 2-MBO with 2-chloro acetyl chloride to give 2-chloroacetyl thio benzoxazole (2), the product was treated with phenyl hydrazine to give 2-phenyl hydrazide acetyl thio benzoxazole (3). The new derivatives (4-13) were synthesized by reaction of 2-phenyl hydrazide acetyl thio benzoxazole (3) with different aromatic aldehydes in the presence of acetic acid. The compound (2) was treated with hydrazine hydrate to give product (14) then treated with different aromatic aldehydes in the presence of glacial acetic acid to give Schiff bases derivatives (15-24). Structure of all the prepared compounds confirmation were proved

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Publication Date
Fri Nov 24 2023
Journal Name
Iraqi Journal Of Science
Synthesis and characterization of some New Derivatives from 2- Mercaptobenzothiazole
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In this work 2- mercaptobenzothiazole ( 2-MBT ) and some of its derivatives(1, 14 ,27) were prepared by using home made Auto clave .The synthesis involve treatment of 2- MBT or some of its derivatives with chloro acetyl chloride to give 1- chloro acetyl -2- MBT or the corresponding derivatives (2,15,28) . the product was treated with phenyl hydrazine to give the phenyl hydrazide derivatives (3,16,29) . The new derivatives(4-13, 17-26,30-39) were synthesized by reaction of the phenyl hydrazide derivatives with different aromatic aldehydes in the presence of Acetic Acid . Structure of all the prepared compounds confirmation were proved using FTIR , elemental analysis (C .H .N .S ) in addition to melting points.

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Publication Date
Mon Aug 07 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Preliminary Pharmacological Evaluation of Some New Triazole Derivatives
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  On the basis of the results which was previously obtained from the structural and the theoretical studies on ~-adrenergic drugs, a series of 2-propanolamine derivatives containing triazole moiety have been prepared and evaluated for their cardiovascular activity . These derivatives were tested by using spontaneously-beating right atria of albino rats.

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