Palestinian Medical and Pharmaceutical Journal (Pal. Med. Pharm. J.)

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Palestinian Medical and Pharmaceutical Journal (Pal. Med. Pharm. J.) Indexed in Scopus since 2022
CiteScore 1.0
Indexed since 2022
First decision 7 Days
Submission to acceptance 45 Days
Acceptance to publication 14 Days
Acceptance rate 8%

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Palestinian Medical and Pharmaceutical Journal (Pal. Med. Pharm. J.) Open directory record
Original full research article

Synthesis, Characterization, Molecular Docking, and Preliminary Antimicrobial Evaluation of Thiazolidinone Derivatives

Published
2024-06-01
Pages
181 - 192
Full text

Keywords

  • Antimicrobial resistance
  • Thiazolidine-4-One
  • Molecular docking
  • Drug discovery
  • Antimicrobial agents
  • Com-puter-aided drug design

Abstract

Several derivatives carrying thiazolidine-4-one pharmacophore were prepared to evaluate their antimicrobial activities. The set of compounds were shown to possess potential activities as determined by molecular docking studies for both candidal (14-alpha demethylase) and bacterial enzymes (Penicillin binding protein of E. coli). In vitro antimicrobial activities were also performed to confirm the molecular docking results. Molecular characterization by spec-tral techniques (FT-IR, 13C NMR and 1H NMR) was carried out to confirm the identity of the synthesized compounds. The synthesized compounds were evaluated for antibacterial and anticandidal activity by comparing them with the reference drugs (positive controls) ceftriax-one and fluconazole respectively. Four bacterial species (Klebsiella pneumonia, Escherichia coli, Staphylococcus epidermis, Staphylococcus aureus) and one fungal species (Candida albicans) were inoculated into petri dishes and were expose to the synthesized compounds by well diffusion method. The series of the proposed compounds were successfully synthesized and some of them were proven to have antibacterial activities comparable to the reference drug. Particularly, the compounds 2c and 2a posessed activities against K. pneumomia being higher than ceftriaxone with average inhibition zone diameters of 17 mm and 16 mm at highest concentration respectively. Compound 2b was effective against E. Coli also yielding higher activity than ceftriaxone achieving an average diameter of 17 mm at the highest concentration.

Article history

Received
2023-06-22
Accepted
2023-08-26
Available online
2024-06-01
بحث أصيل كامل

Synthesis, Characterization, Molecular Docking, and Preliminary Antimicrobial Evaluation of Thiazolidinone Derivatives

Published
2024-06-01
الصفحات
181 - 192
البحث كاملا

الكلمات الإفتتاحية

  • Antimicrobial resistance
  • Thiazolidine-4-One
  • Molecular docking
  • Drug discovery
  • Antimicrobial agents
  • Com-puter-aided drug design

الملخص

Several derivatives carrying thiazolidine-4-one pharmacophore were prepared to evaluate their antimicrobial activities. The set of compounds were shown to possess potential activities as determined by molecular docking studies for both candidal (14-alpha demethylase) and bacterial enzymes (Penicillin binding protein of E. coli). In vitro antimicrobial activities were also performed to confirm the molecular docking results. Molecular characterization by spec-tral techniques (FT-IR, 13C NMR and 1H NMR) was carried out to confirm the identity of the synthesized compounds. The synthesized compounds were evaluated for antibacterial and anticandidal activity by comparing them with the reference drugs (positive controls) ceftriax-one and fluconazole respectively. Four bacterial species (Klebsiella pneumonia, Escherichia coli, Staphylococcus epidermis, Staphylococcus aureus) and one fungal species (Candida albicans) were inoculated into petri dishes and were expose to the synthesized compounds by well diffusion method. The series of the proposed compounds were successfully synthesized and some of them were proven to have antibacterial activities comparable to the reference drug. Particularly, the compounds 2c and 2a posessed activities against K. pneumomia being higher than ceftriaxone with average inhibition zone diameters of 17 mm and 16 mm at highest concentration respectively. Compound 2b was effective against E. Coli also yielding higher activity than ceftriaxone achieving an average diameter of 17 mm at the highest concentration.

Article history

تاريخ التسليم
2023-06-22
تاريخ القبول
2023-08-26
Available online
2024-06-01