دورية أكاديمية
Mycobacterium tuberculosis lysine-ɛ-aminotransferase a potential target in dormancy: Benzothiazole based inhibitors.
| العنوان: | Mycobacterium tuberculosis lysine-ɛ-aminotransferase a potential target in dormancy: Benzothiazole based inhibitors. |
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| المؤلفون: | Reshma RS; Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Hyderabad 500078, India., Jeankumar VU; Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Hyderabad 500078, India., Kapoor N; Burnett School of Biomedical Sciences, College of Medicine, University of Central Florida, Orlando, FL, USA., Saxena S; Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Hyderabad 500078, India., Bobesh KA; Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Hyderabad 500078, India., Vachaspathy AR; Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Hyderabad 500078, India., Kolattukudy PE; Burnett School of Biomedical Sciences, College of Medicine, University of Central Florida, Orlando, FL, USA., Sriram D; Department of Pharmacy, Birla Institute of Technology & Science-Pilani, Hyderabad Campus, Hyderabad 500078, India. Electronic address: dsriram@hyderabad.bits-pilani.ac.in. |
| المصدر: | Bioorganic & medicinal chemistry [Bioorg Med Chem] 2017 May 15; Vol. 25 (10), pp. 2761-2771. Date of Electronic Publication: 2017 Mar 27. |
| نوع المنشور: | Journal Article; Research Support, Non-U.S. Gov't |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier Science Country of Publication: England NLM ID: 9413298 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3391 (Electronic) Linking ISSN: 09680896 NLM ISO Abbreviation: Bioorg Med Chem Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: Oxford : Elsevier Science Original Publication: Oxford : New York : Pergamon Press, c1993- |
| مواضيع طبية MeSH: | Antitubercular Agents/*chemistry , Bacterial Proteins/*antagonists & inhibitors , Benzothiazoles/*chemistry , Enzyme Inhibitors/*chemistry , Mycobacterium tuberculosis/*metabolism , Transaminases/*antagonists & inhibitors, Antitubercular Agents/metabolism ; Antitubercular Agents/pharmacology ; Bacterial Proteins/metabolism ; Benzothiazoles/metabolism ; Benzothiazoles/pharmacology ; Binding Sites ; Catalytic Domain ; Drug Design ; Enzyme Inhibitors/metabolism ; Enzyme Inhibitors/pharmacology ; Molecular Docking Simulation ; Mycobacterium tuberculosis/drug effects ; Structure-Activity Relationship ; Transaminases/metabolism |
| مستخلص: | MTB lysine-ɛ-aminotransferase (LAT) was found to play a crucial role in persistence and antibiotic tolerance. LAT serves as a potential target in the management of latent tuberculosis. In present work we attempted to derivatize the benzothiazole lead identified through high throughput virtual screening of Birla Institute of Technology and Science in house database. For Structure activity relationship purpose 22 derivatives were synthesized and characterized. Among synthesized compounds, eight compounds were found to be more efficacious in terms of LAT inhibition when compared to lead compound (IC (Copyright © 2017 Elsevier Ltd. All rights reserved.) |
| فهرسة مساهمة: | Keywords: 3D granuloma model; Benzothiazole derivatives; Dormancy; Lysine-ɛ amino transferase; Mycobacterium tuberculosis |
| المشرفين على المادة: | 0 (Antitubercular Agents) 0 (Bacterial Proteins) 0 (Benzothiazoles) 0 (Enzyme Inhibitors) EC 2.6.1.- (Transaminases) |
| تواريخ الأحداث: | Date Created: 20170409 Date Completed: 20170426 Latest Revision: 20171208 |
| رمز التحديث: | 20240628 |
| DOI: | 10.1016/j.bmc.2017.03.053 |
| PMID: | 28389113 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1464-3391 |
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| DOI: | 10.1016/j.bmc.2017.03.053 |