Abstract
The challenges in preventing and controlling tuberculosis are further complicated by the deadly rise of multidrug- resistant tuberculosis (MDR-TB). Recognizing the seriousness of the situation, we initiated a program to screen new agents that would satisfy these unmet needs and have a favorable safety profile. Mycobacteria are well known for their lipid-rich properties. In Mycobacterium tuberculosis, mycolic acid in particular has been established the wall component related to the pathogenesis in the host. There are approximately 250 identified genes related to biosynthesis of the lipid turnover that contain InhA, the main target of isoniazid. Thus, the logical approach for developing a chemotherapy agent against tubercle bacilli included screening compounds that could inhibit the biosyntheses of mycolic acid and that had a novel chemical structure to ensure improved efficacy against MDR-TB. Some of the screening systems established for those purposes and some of the candidates are outlined.
Keywords: Tuberculosis, mycolic acid inhibitor, nitrodehydroimidazooxazole, mycolic acid, BRM test
Current Topics in Medicinal Chemistry
Title: Screening for Novel Antituberculosis Agents that are Effective Against Multidrug Resistant Tuberculosis
Volume: 7 Issue: 5
Author(s): Makoto Matsumoto, Hiroyuki Hashizume, Hidetsugu Tsubouchi, Hirofumi Sasaki, Motohiro Itotani, Hideaki Kuroda, Tatsuo Tomishige, Masanori Kawasaki and Makoto Komatsu
Affiliation:
Keywords: Tuberculosis, mycolic acid inhibitor, nitrodehydroimidazooxazole, mycolic acid, BRM test
Abstract: The challenges in preventing and controlling tuberculosis are further complicated by the deadly rise of multidrug- resistant tuberculosis (MDR-TB). Recognizing the seriousness of the situation, we initiated a program to screen new agents that would satisfy these unmet needs and have a favorable safety profile. Mycobacteria are well known for their lipid-rich properties. In Mycobacterium tuberculosis, mycolic acid in particular has been established the wall component related to the pathogenesis in the host. There are approximately 250 identified genes related to biosynthesis of the lipid turnover that contain InhA, the main target of isoniazid. Thus, the logical approach for developing a chemotherapy agent against tubercle bacilli included screening compounds that could inhibit the biosyntheses of mycolic acid and that had a novel chemical structure to ensure improved efficacy against MDR-TB. Some of the screening systems established for those purposes and some of the candidates are outlined.
Export Options
About this article
Cite this article as:
Matsumoto Makoto, Hashizume Hiroyuki, Tsubouchi Hidetsugu, Sasaki Hirofumi, Itotani Motohiro, Kuroda Hideaki, Tomishige Tatsuo, Kawasaki Masanori and Komatsu Makoto, Screening for Novel Antituberculosis Agents that are Effective Against Multidrug Resistant Tuberculosis, Current Topics in Medicinal Chemistry 2007; 7 (5) . https://dx.doi.org/10.2174/156802607780059727
DOI https://dx.doi.org/10.2174/156802607780059727 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Idiopathic Transverse Myelitis and Neuromyelitis Optica: Clinical Profiles,Pathophysiology and Therapeutic Choices
Current Neuropharmacology Tuberculosis Vaccines: Hopes and Hurdles
Infectious Disorders - Drug Targets Synthesis and Antibacterial Properties of Oxazolidinones and Oxazinanones
Anti-Infective Agents in Medicinal Chemistry Adaptors in Toll-Like Receptor Signaling and their Potential as Therapeutic Targets
Current Drug Targets Editorial (Thematic Issue: Biomarkers of Impaired Innate and Adaptive Immunity in Health and Disease)
Current Immunology Reviews (Discontinued) Evaluation of Arthritis in Hanseniase
Current Rheumatology Reviews Potential Triazole-based Molecules for the Treatment of Neglected Diseases
Current Medicinal Chemistry Chronic Diseases and COVID-19: A Review
Endocrine, Metabolic & Immune Disorders - Drug Targets Advanced in Silico Methods for the Development of Anti- Leishmaniasis and Anti-Trypanosomiasis Agents
Current Medicinal Chemistry Applications and Case Studies of the Next-Generation Sequencing Technologies in Food, Nutrition and Agriculture
Recent Patents on Food, Nutrition & Agriculture Triazole-linked Chalcone and Flavone Hybrid Compounds Based on AZT Exhibiting In Vitro Anti-Cancer Activity
Letters in Drug Design & Discovery Biodegradable Polymeric Nanoparticles as the Delivery Carrier for Drug
Current Drug Delivery Revisit: Eaton’s Reagent Catalyzed Synthesis of Mono and Bis-Chalcone Derivatives
Letters in Organic Chemistry Insights in Nanoparticle-Bacterium Interactions: New Frontiers to Bypass Bacterial Resistance to Antibiotics
Current Pharmaceutical Design Polysaccharides to Combat Viruses (COVID-19) and Microbes: New updates
Current Molecular Pharmacology Drug Repurposing: Translational Pharmacology, Chemistry, Computers and the Clinic
Current Topics in Medicinal Chemistry Synthesis and Biological Activity of Chiral Dihydropyrazole: Potential Lead for Drug Design
Mini-Reviews in Medicinal Chemistry Artificial Intelligence Approaches for Rational Drug Design and Discovery
Current Pharmaceutical Design Identification of Selectivity Determinants in CYP Monooxygenases by Modelling and Systematic Analysis of Sequence and Structure
Current Drug Metabolism Biologic Therapy in Psoriasis: Safety Profile
Current Drug Safety