Tackling Microbial Resistance with Isatin-Decorated Thiazole Derivatives: Design, Synthesis, and in vitro Evaluation of Antimicrobial and Antibiofilm Activity
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 Universi...
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ftdoajarticles:oai:doaj.org/article:d1f6dc596e464683ac8b3a5e0ce753b3 2023-05-15T18:12:00+02:00 Tackling Microbial Resistance with Isatin-Decorated Thiazole Derivatives: Design, Synthesis, and in vitro Evaluation of Antimicrobial and Antibiofilm Activity Kassab RM Al-Hussain SA Elleboudy NS Albohy A Zaki MEA Abouzid KAM Muhammad ZA 2022-08-01T00:00:00Z https://doaj.org/article/d1f6dc596e464683ac8b3a5e0ce753b3 EN eng Dove Medical Press https://www.dovepress.com/tackling-microbial-resistance-with-isatin-decorated-thiazole-derivativ-peer-reviewed-fulltext-article-DDDT https://doaj.org/toc/1177-8881 1177-8881 https://doaj.org/article/d1f6dc596e464683ac8b3a5e0ce753b3 Drug Design, Development and Therapy, Vol Volume 16, Pp 2817-2832 (2022) 5-bromoisatin thiosemicarbazone hydrazonoyl chlorides thiazoles tyrosyl-trna synthetases (tyrrs) inhibitors antimicrobial molecular docking mrsa antibiofilm Therapeutics. Pharmacology RM1-950 article 2022 ftdoajarticles 2022-12-31T01:09:12Z 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 +20101-336-2594, Fax +20-25685799, Email rkassab@sci.cu.edu.eg Sami A Al-Hussain, Department of Chemistry, Faculty of Science, Imam Mohammad Ibn Saud Islamic University (IMSIU), Riyadh, 11623, Saudi Arabia, Email sahussain@imamu.edu.saIntroduction: 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 ... Article in Journal/Newspaper sami Directory of Open Access Journals: DOAJ Articles |
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Directory of Open Access Journals: DOAJ Articles |
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English |
topic |
5-bromoisatin thiosemicarbazone hydrazonoyl chlorides thiazoles tyrosyl-trna synthetases (tyrrs) inhibitors antimicrobial molecular docking mrsa antibiofilm Therapeutics. Pharmacology RM1-950 |
spellingShingle |
5-bromoisatin thiosemicarbazone hydrazonoyl chlorides thiazoles tyrosyl-trna synthetases (tyrrs) inhibitors antimicrobial molecular docking mrsa antibiofilm Therapeutics. Pharmacology RM1-950 Kassab RM Al-Hussain SA Elleboudy NS Albohy A Zaki MEA Abouzid KAM Muhammad ZA Tackling Microbial Resistance with Isatin-Decorated Thiazole Derivatives: Design, Synthesis, and in vitro Evaluation of Antimicrobial and Antibiofilm Activity |
topic_facet |
5-bromoisatin thiosemicarbazone hydrazonoyl chlorides thiazoles tyrosyl-trna synthetases (tyrrs) inhibitors antimicrobial molecular docking mrsa antibiofilm Therapeutics. Pharmacology RM1-950 |
description |
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 +20101-336-2594, Fax +20-25685799, Email rkassab@sci.cu.edu.eg Sami A Al-Hussain, Department of Chemistry, Faculty of Science, Imam Mohammad Ibn Saud Islamic University (IMSIU), Riyadh, 11623, Saudi Arabia, Email sahussain@imamu.edu.saIntroduction: 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 ... |
format |
Article in Journal/Newspaper |
author |
Kassab RM Al-Hussain SA Elleboudy NS Albohy A Zaki MEA Abouzid KAM Muhammad ZA |
author_facet |
Kassab RM Al-Hussain SA Elleboudy NS Albohy A Zaki MEA Abouzid KAM Muhammad ZA |
author_sort |
Kassab RM |
title |
Tackling Microbial Resistance with Isatin-Decorated Thiazole Derivatives: Design, Synthesis, and in vitro Evaluation of Antimicrobial and Antibiofilm Activity |
title_short |
Tackling Microbial Resistance with Isatin-Decorated Thiazole Derivatives: Design, Synthesis, and in vitro Evaluation of Antimicrobial and Antibiofilm Activity |
title_full |
Tackling Microbial Resistance with Isatin-Decorated Thiazole Derivatives: Design, Synthesis, and in vitro Evaluation of Antimicrobial and Antibiofilm Activity |
title_fullStr |
Tackling Microbial Resistance with Isatin-Decorated Thiazole Derivatives: Design, Synthesis, and in vitro Evaluation of Antimicrobial and Antibiofilm Activity |
title_full_unstemmed |
Tackling Microbial Resistance with Isatin-Decorated Thiazole Derivatives: Design, Synthesis, and in vitro Evaluation of Antimicrobial and Antibiofilm Activity |
title_sort |
tackling microbial resistance with isatin-decorated thiazole derivatives: design, synthesis, and in vitro evaluation of antimicrobial and antibiofilm activity |
publisher |
Dove Medical Press |
publishDate |
2022 |
url |
https://doaj.org/article/d1f6dc596e464683ac8b3a5e0ce753b3 |
genre |
sami |
genre_facet |
sami |
op_source |
Drug Design, Development and Therapy, Vol Volume 16, Pp 2817-2832 (2022) |
op_relation |
https://www.dovepress.com/tackling-microbial-resistance-with-isatin-decorated-thiazole-derivativ-peer-reviewed-fulltext-article-DDDT https://doaj.org/toc/1177-8881 1177-8881 https://doaj.org/article/d1f6dc596e464683ac8b3a5e0ce753b3 |
_version_ |
1766184576249495552 |