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bijps-452
Synthesis of Coumarin Derivatives Coupled to Amino Acid Esters and Studying their Biological Activity as Antimicrobial Agents
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A series of coumarin derivatives linked to amino acid ester side chains were synthesized and evaluated of their antibacterial and antifungal activity. The coumarin derivatives was alkylated by the ethyl bromoacetate and then using potassium carbonate to get alkylated hymecromone. Conventional solution method for amide bond formation was used as a coupling method between the carboxy-protected amino acids with acetic acid side chain of coumarin derivatives. The DCC/ HOBt coupling reagents were used for peptide bond formation. The proposed analogues were successfully synthesized and their structural formulas were consistent with the proposed structures as they were proved and characterized by thin layer chromatography (TLC), melting point, infrared spectroscopy (IR), and elemental microanalysis (CHN).

Key words: coumarin, amino acid, coumarin antimicrobialal activity.

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Publication Date
Sat Dec 01 2018
Journal Name
Journal Of Pharmaceutical Sciences And Research
Synthesis and biological activity of new esters derived from D-fructose-containing isoxazole moiety
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Background: Isoxazoles are an important class of five-membered unsaturated heterocyclic compounds. They show several applications in diverse areas such as pharmaceuticals, agrochemistry and industry. Isoxazoles are also found in natural sources showing insecticidal, plant growth regulation and pigment functions. Current study was conducted for synthesis of twenty five new Isoxazole derivatives and to evaluate the in vitro antibacterial activities of these derivatives. Methods: Benzaldoxime and their substituted [I] ae were prepared via addition-elimination reactions between aromatic aldehyde and hydroxylamine hydrochloride. In a second step, para-or meta-substituted benzaldoximes [I] ae were reacted with N-chlorosucceinimide in DMF to yield

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Publication Date
Tue Apr 30 2024
Journal Name
Iraqi Journal Of Science
Synthesis, Characterization and Antimicrobial Evaluation for New Esters Derivatives Containing Two 1, 3, 4-Oxadiazole Units
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     This work includes the synthesis of new ester compounds containing two 1,3,4-oxadiazole rings, 15a-c and 16a-c. This was done over seven steps, starting with p-acetamido-phenol 1 and 2-mercaptobenzoimidazole 2. The structure of the products was determined using FT-IR, 1H NMR, and mass spectroscopy. The evaluation of the antimicrobial activities of some prepared compounds was achieved against four types of bacteria (two types of gram-positive bacteria; Staphylococcus aureus and Bacillus subtilis, and two types of gram-negative bacteria, Pseudomonas aeruginosa and E. Coli), as well as against one types of fungus (C. albino). The results show moderate activit against the study bacteria, and the theoretical analysis of the toxi

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Publication Date
Tue Jul 01 2008
Journal Name
D
Synthesis and Identification of Some New Derivatives of Schiff bases Compounds and study their Biological activity
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A new series of Schiff bases compounds , containing an azomethine linkage was synthesized and expected to be biologically active .The structures of these compounds were identified by IR , Uv/vis spectra , melting points and followed by T.L.C.The biological activity of these compounds was studied

Publication Date
Mon Jun 08 2020
Journal Name
Systematic Review Pharmacy
Synthesis and Biological Activity of Some New Thiazolidinone Derivatives
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The compound [G1] was prepared from the reaction of thiosemicarbazide with para-hydroxyphenylmethyl ketone in ethanol as a solvent. Then by sequence reactions prepared [G2] and [G3] compounds. The compound [G4] reaction with ethyl acetoacetoneto synthesized compound [G6] and acetyl acetone to synthesized compound [G5]. Reaction the [G3] with two different types of aldehydes in the present of pipredine to form new alkenes compounds [G7]and [G8].The compound [G3] reacted with hydrazine hydrate to formation[G4] with present the hydrazine hydrade 80% in (10) ml of absolute ethanol. Latter the compound [G4]reacted with different aldehydes with present the glacial acetic acid and the solvent was ethanol to formed the Schiff bases compounds[G9] an

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Publication Date
Thu Mar 19 2020
Journal Name
Systematic Review Pharmacy
Synthesis and Biological Activity of Some New Thiazolidinone Derivatives
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The compound [G1] was prepared from the reaction of thiosemicarbazide with para-hydroxyphenylmethyl ketone in ethanol as a solvent. Then by sequence reactions prepared [G2] and [G3] compounds. The compound [G4] reaction with ethyl acetoacetoneto synthesized compound [G6] and acetyl acetone to synthesized compound [G5]. Reaction the [G3] with two different types of aldehydes in the present of pipredine to form new alkenes compounds [G7]and [G8].The compound [G3] reacted with hydrazine hydrate to formation[G4] with present the hydrazine hydrade 80% in (10) ml of absolute ethanol. Latter the compound [G4]reacted with different aldehydes with present the glacial acetic acid and the solvent was ethanol to formed the Schiff bases compounds[G9] an

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Publication Date
Mon Jul 01 2019
Journal Name
J. Pharm. Sci. & Res.
Methods of Synthesis Phthalimide Derivatives and Biological Activity-Review
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Phthalimide formation of Phthalic anhydride with various amines using microwave or without a method with the difference of the catalyst used in a prepared Phthalimide, either structure general are C6H4CONRCO and used as starting materials in synthesis several compounds derivative phthalimides are an important compounds because spectrum wide biological activities including Antimicrobial activity, anticonvulsant activity, Anti-inflammatory activity,Analgesic activity, Anti- influenza activity and Thromboxane inhibitory activity

Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Preliminary Antimicrobial Study of 2-Amino-5-Mercapto-1,3,4-Thiadiazole Derivatives
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Nitrogen heterocycles are of a special interest because they constitute an important class of natural and non natural products, many of which exhibit useful biological activities.Among these nitrogen heterocycles are 1, 3, 4-thiadiazole containing compounds. The therapeutic effects of these derivatives have been well studied for a number of pathological conditions including inflammation, pain, or hypertension. Moreover, synthesis of thiadiazoles has attracted wide-spread attention due to their diverse applications as antibacterial, anticancer, antifungal anti-inflammatory and antidepressant agents.According to this information’s new derivatives of 1, 3, 4-thiadiazole were designed and synthesized and in the hope of having some act

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Publication Date
Fri Jun 21 2024
Journal Name
Pharmacia
Synthesis and biological activity evaluation of new isatin-gallate hybrids as antioxidant and anticancer agents (in vitro) and in silico study as anticancer agents and coronavirus inhibitors
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Background: The hybrid compounds hold promise for developing novel pharmaceuticals, potentially exhibiting greater activity, mainly against viruses and cancer diseases, than their components.

Objective: In this study, researchers explored the potential synergistic effects of hybrid molecules by designing and synthesizing a series of isatin-gallate hybrids, denoted as N’-(5-substituted-2-oxoindolin-3-ylidene)-3,4,5-trihydroxybenzohydrazide (3a–d).

Methods: Isatin-gallate hybrids (3a–d) were synthesized by reacting gallic hydrazide with each of the isatin analogs (2a–d). The structures of all produced comp

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Publication Date
Thu Jun 30 2022
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization of New Sulfamethoxazole Derivatives containing β-lactam Ring and Preliminary Evaluation of their Antimicrobial Activity
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Sulfamethoxazole (SMX) is the most significant antibiotic in the sulfonamide family. It was chosen as the representative of this category because of its widespread use. Starting with sulfamethoxazole, a new series of 2-Azetidinone (M1-M6) was synthesized, the structure of these new derivatives was confirmed using spectral methods, starting with the synthesis of Schiff’s bases by reflux of different aromatic benzaldehydes, separately, with Sulfamethoxazole in ethanol with few drops of acetic acid. The final compounds were obtained by ketene-imine synthesis of β-lactam using chloroacetyl chloride. The designed chemicals’ synthesis has been completed successfully. Physical parameters (melting points and Rf values), Fourier transfo

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Publication Date
Wed Sep 02 2020
Journal Name
International Journal Of Drug Delivery Technology
Synthesis of Levofloxacin Derivatives with some Amines and their Complexes with Copper(II) Salts and Evaluation of their Biological Activity
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Levofloxacin belongs to the fluoroquinolone family; it is a potent broad-spectrum bactericidal agent. The pharmacophore required for significant antibacterial activity is the C-3 carboxylic acid group and the 4-pyridine ring with the C-4 carbonyl group, into which binding to the DNA bases occur. In this work, we tried to show that by masking the carboxyl group through amide formation using certain amines to form levofloxacin carboxamides, an interesting activity is kept. Levofloxacin carboxamides on the C-3 group were prepared, followed by the formation of their copper complexes. The target compounds were characterized by FT-IR, elemental analysis. The antimicrobial activity of the target compounds was evaluated and showed satisfactory resu

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