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Synthesis, Characterization, Molecular Docking, ADMET Study, and Antimicrobial Evaluation of New Mannich Bases of Isatin–Thiazole Imine Bases
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Background: The isatin molecule is present in many natural substances, including plants and animals, and is used to prepare compounds with various biological activities. Objectives: To synthesize a new series of isatin derivatives with the expectation that they will have antimicrobial activity. Methods: Thiazole Schiff bases were synthesized from various Mannich bases of isatin to evaluate their antimicrobial properties. Initially, Mannich bases (2a–e) were synthesized by reacting isatin with formaldehyde and different secondary amines. Subsequently, they were treated with 2-aminothiazole to yield the final compounds (3a–e). Spectroscopic characterization was done via FT-IR and 1H-NMR. The antimicrobial screening was conducted on all derivatives. Molecular docking and ADMET analysis were performed on the final compounds, comparing them with standard drugs (ciprofloxacin and fluconazole). Results: The antimicrobial activity was assessed on two Gram-positive bacteria, Staphylococcus aureus and Bacillus licheniformis; two Gram-negative bacteria, Escherichia coli and Acinetobacter baumannii; and one fungus species, Candida albicans. Molecular docking has recorded higher docking scores for 3d and 3e compared to ciprofloxacin and fluconazole. The virtually active molecules showed an adequate drug-like profile and desired pharmacokinetic properties in the ADMET analysis. Conclusions: Most derivatives displayed significant antimicrobial activity, with compound 3e being the most active, followed by compound 3b. Molecular docking revealed higher scores for compound 3e compared to fluconazole and for compounds 3d and 3e compared to ciprofloxacin. ADMET analysis of compound 3e showed excellent absorption, consistent with its strong GIT absorption.

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
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 struct

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Publication Date
Mon Jun 30 2003
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Study of the Drying of Ethanol using Zeolite Molecular Sieves
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Publication Date
Mon Mar 01 2021
Journal Name
Journal Of Physics: Conference Series
Synthesis and study the liquid crystalline properties of new compounds containing 5-methyl-2,4-dihydro-3H-pyrazol-3-one
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Abstract<p>The new compounds of pyrazolines were synthesized from the reaction of different acid hydrazide with ethylacetoacetate and ethanol under reflux. These compounds were obtained from many sequence reactions. The 4-acetyl-5-methyl-2,4-dihydro-3H-pyrazol-3-one compounds synthesized from the reaction of 5-methyl-2,4-dihydro-3H-pyrazol-3-one with acetyl chloride in calcium hydroxide and 1,4-dioxane. Finaly, Schiff bases were prepared via condensation reaction of products of mono- and tri ketone derivatives[IV]<sub>a, b</sub> with phenyl hydrazines as presented in (Scheme 1, 2). The synthesized compounds were identification by using FTIR, NMR and Mass spectroscopy (of some of them).</p> ... Show More
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Publication Date
Sat Jun 01 2024
Journal Name
Russian Journal Of Bioorganic Chemistry
Synthesis and Study the Biological Activity of Some New Pyrazole Compounds Containing 1,3,4-Oxadiazole Unite Through Vilsmeier–Haack Reaction
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Publication Date
Mon Mar 27 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of New Cephalosporins of Expected Improved Activity and Resistance Against -Lactamases
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The development of new cephalosporins with improved activity against resistant microbes, such as, MRSA (methicillin resistant Staph. aureus), P. aeruginosa, is of high potential. Chemical synthesis of two new series of thiadiazole linked to cysteine (series 1) and cephalosporins containing thiadiazole linked to cysteine through disulfide bond (series 2) were achieved. The chemical structures of the synthesized compounds were confirmed using spectral (FT-IR, 1H-NMR) and elemental microanalysis. The incorporation of privileged chemical moieties, such as, thiadiazole, Schiff base, cysteine and sulfonamide, has been found to have great contribution to the antimicrobial activities. Compounds of series 1 (1

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Publication Date
Fri Jan 01 2021
Journal Name
Research Journal Of Pharmacy And Technology
Bacteriological and molecular study on S. Aureus bacteria Atala, M.L.
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Publication Date
Mon Sep 25 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Preparation and Characterization of A New Nano-scaled Material Composed of Bentonite-Polyethylenglycophthalate
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   In this study a new composite material have been prepared and characterized through polymerization of ethylene glycol located between the Bentonite layers with phthalic anhydride. The results showed that the polymer binds with the structure of clay through hydrogen bonding also the polymerization process led to shatter of the three-dimension crystal structure of the clay and isolating layers in the form of nano-scale two-dimensional sheets, the polymer growth around the clay isolated layers work to increase the size particles at microscopic scale.                              &

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Publication Date
Fri Jul 05 2013
Journal Name
Pharmacie Globale International Journal Of Comprehensive Pharmacy
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

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Publication Date
Sun Dec 04 2016
Journal Name
Baghdad Science Journal
Synthesis of new Polyimides Derived from 4- minoantipyrine
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In the present study, new five polymers of acryloyl chloride have been synthesized by reaction 4-aminoantipyrine with many substituted acid chloride (A-E). Then condensation of polyacryloyl chloride with the product in one step (A-E), in a suitable solvent in the presence amount of (Et3N) to obtain new polyimides(A1-E5). The prepared compounds were characterized by UV. FT-IR, 1H-NMR and 13C-NMR spectroscopy and measuring of other physical properties such as softening point, melting point and solublities.

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Publication Date
Mon Sep 30 2002
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
The New Synthesis of Potassium-Exchange Zeolite A
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