Tackling Microbial Resistance with Isatin-Decorated Thiazole Derivatives: Design, Synthesis, and in vitro Evaluation of Antimicrobial and Antibiofilm Activity

• Main Authors: Kassab RM, Al-Hussain SA, Elleboudy NS, Albohy A, Zaki MEA, Abouzid KAM, Muhammad ZA
• Format: Article in Journal/Newspaper
• Language: English
• Published: Dove Medical Press 2022
• Subjects: 5-bromoisatin; thiosemicarbazone; hydrazonoyl chlorides; thiazoles; tyrosyl-trna synthetases (tyrrs) inhibitors; antimicrobial; molecular docking; mrsa; antibiofilm; Therapeutics. Pharmacology; RM1-950; sami
• Online Access: https://doaj.org/article/d1f6dc596e464683ac8b3a5e0ce753b3

Refaie M Kassab,1 Sami A Al-Hussain,2 Nooran S Elleboudy,3 Amgad Albohy,4 Magdi EA Zaki,2 Khaled AM Abouzid,5,6 Zeinab A Muhammad7 1Department of Chemistry, Faculty of Science, Cairo University, Giza, 12613, Egypt; 2Department of Chemistry, Faculty of Science, Imam Mohammad Ibn Saud Islamic University (IMSIU), Riyadh, 11623, Saudi Arabia; 3Department of Microbiology and Immunology, The Faculty of Pharmacy, Ain Shams University, Cairo, 11566, Egypt; 4Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The British University in Egypt (BUE), Cairo, 11837, Egypt; 5Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ain Shams University, Cairo, 11566, Egypt; 6Department of Organic and Medicinal Chemistry, Faculty of Pharmacy, University of Sadat City, Sadat City, Egypt; 7Department of Organic Chemistry, National Organization for Drug Control and Research (NODCAR), Giza, 12311, EgyptCorrespondence: Refaie M Kassab, Department of Chemistry, Faculty of Science, Cairo University, Giza, 12613, Egypt, Tel [phone], Fax [phone], Email [e-mail] Sami A Al-Hussain, Department of Chemistry, Faculty of Science, Imam Mohammad Ibn Saud Islamic University (IMSIU), Riyadh, 11623, Saudi Arabia, Email [e-mail]: Antibiotic resistance is a global threat that has been increasing recently, especially with antibiotic overuse and misuse. The search for new antibiotics is becoming more and more indispensable.Methods: Design and synthesis of isatin derivatives as surrogates of SB-239629, a bacterial tyrosine-tRNA synthetases (TyrRS) inhibitor. The newly synthesized compounds were screened for their antimicrobial and antibiofilm activities. Docking studies were used to investigate potential binding modes of these compounds with TyrRS.Results and Discussion: Newly synthesized isatin-decorated thiazole derivatives (7b, 7d, and 14b) have shown potent antimicrobial activities against E. coli, a representative of gram-negative bacteria. Also, 7f showed the best activity against ...