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Ammar H. Al-Dujaili
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Medicine & Pharmacology

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Synthesis, Characterization and Biological Activity of New Ester Containing Azo Group Derived From 2-Amino-1, 3, 4-Thiadiazoline Derivatives Ammar H. Al-Dujaili
Journal of Global Pharma Technology Volume 10 Issue 05: (2018) May2018
Publisher : Journal of Global Pharma Technology

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Abstract

New azo compounds derived from 2-amino-1,3,4-thiadiazolines were synthesized. The cyclization reaction of thiosemicarbazones [I]a,b with the acetic anhydride lead to formation of 1,3,4-thiadiazoline compounds [II]a,b. Compounds[II]a,b were converted to 2-amino-1,3,4- thiadiazolines [III]a,b by hydrolysis of amide group using hydrazine hydrate. The new azo compounds [IV]a,b were synthesized via converted  the amino group of [III]a,b to diazonium salt, follow by the reaction with 4-hydroxyphenol. Finally the ester compounds [V]a-f was synthesized from the reaction of azo compounds with suitable carboxylic acid chloride. The synthesized compounds were characterized by elemental analysis, FTIR, 1HNMR and mass spectroscopy. All these compounds were evaluated for antibacterial activity against Staphylococcus aureus, Bacillius Subtilis, Escherichia coli and Pseudomonas aeruginosa by disk diffusion method and for antifungal activity against Aspergillus niger in Sabouraudʼs dextrose agar medium. Amoxicillin and fluconazole were used as standard drugs for Gram positive, Gram negative and antifungal activity, respectively. Most of the compounds have shown significant antibacterial and antifungal activity when compared with the standard antimicrobial agents.Keywords: 1, 3, 4-Thiadiazoline; Ester compounds; Azo compounds; Antibacterial activity; Antifungal activity; Disk diffusion.
Synthesis, Characterization and Antimicrobial Activity of Novel Symmetrical and Unsymmetrical Thiadiazole Derivatives as Potential Carbonic Anhydrase Inhibitor in E. Coli Ammar H. Al-Dujaili
Journal of Global Pharma Technology Volume 11 Issue 2: 2019
Publisher : Journal of Global Pharma Technology

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Ten compounds of 2, 5-disubstitutedamido-1, 3, 4-thiadiazole, 3, 5-disubstituted-amido-1, 2, 4-thiadiazole and a Schiff base of 1, 3, 4-thiadiazole derivatives were synthesized. The structures were characterized by elemental analysis and different spectroscopic techniques and their biological activities were evaluated. All the synthesized compounds were screened for their antimicrobial activity against Staphylococcus aureus and Escheriochia coli, and antifungal activity against Candida albicans and a clinical isolate of Candida albicans. Most of the compounds have shown significant antibacterial and antifungal activity. When compared with the standard antimicrobial agents. The induced fit study of Schiff base derivative showed that the compound has potential inhibitory effect on bacterial β carbonic anhydrase with binding score of (-33.681 kJ/mol).Keywords: Thiadiazole;  Antibactrial activity;  Antifungl activity; Amid; Coli.
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