Antitubercular Drug Therapy – Past, Present and Future

K. Purna Nagasree, M. Murali Krishna Kumar  © by the authors

ISBN: 978-1-940366-14-2
Published Date: July, 2016
Pages: 138
Paperback: $95
Publisher: Science Publishing Group
Publication Status: Published
To purchase hard copies of this book, please email: book@sciencepublishinggroup.com
Book Description

This book deals with the introduction of tuberculosis, its worldwide problems, resistance and its posing threat, the available drugs and drug targets. Special emphasis on the threats of multidrug resistance and some methods to overcome it.

Author Introduction

Dr. K. Purna Nagasree DST, Women Scientist -A, Principal Investigator, College of Pharmaceutical Sciences, Andhra University, Visakhapatnam - 530 003, Andhra Pradesh, India.
Dr. M. Murali Krishna Kumar Assistant Professor, College of Pharmaceutical Sciences, Andhra University, Visakhapatnam - 530 003, Andhra Pradesh, India.

Table of Contents
  • The Whole Book

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  • FrontMatter

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  • Chapter 1 Introduction

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    1. 1.1 History of Tuberculosis
    2. 1.1.1 Discovery of the Pathogen
    3. 1.1.2 Tuberculosis: Global Scenario
    4. 1.2 Etiology and Pathophysiology
    5. 1.2.1 M. Tuberculosis (MTB) Complex
    6. 1.2.2 Structural Complexity of M. Tuberculosis Cell Wall
  • Chapter 2 Chemotherapeutic Agents Used for Tuberculosis

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    1. 2.1 History
    2. 2.2 Post Antibiotic ERA
    3. 2.2.1 Streptomycin (SM) and Other Aminoglycoside Antibiotics
    4. 2.2.2 Isoxyl (Thiocarlide) & Thiacetazone
    5. 2.2.3 Isoniazid (INH)
    6. 2.2.4 Pyrazinamide (PZA)
    7. 2.2.5 P-Aminosalicylic Acid (PAS)
    8. 2.2.6 Ethambutol (EMB)
    9. 2.2.7 Cycloserine
    10. 2.2.8 Rifampicin (RMP)
    11. 2.2.9 Fluoroquinolones
    12. 2.3 Conclusions
  • Chapter 3 New Drugs for Treating Tuberculosis in the Clinics and Clinical Trials - An Update

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    1. 3.1 Drugs in Discovery and Development Stages
    2. 3.1.1 Diamines (SQ109)
    3. 3.1.2 Nitroimidazofurans and Nitroimidazopyrans
    4. 3.1.3 Oxazolidinones
    5. 3.1.4 Diarylquinolines (TMC207, SIRTUROTM)
    6. 3.2 Preclinical Agents
    7. 3.2.1 Clofazimine and its Analogues
    8. 3.2.2 Diarylpyrrole Derivatives
    9. 3.2.3 BTZ043 and Its Analogues
    10. 3.2.4 Imidazopyridine Amides
    11. 3.2.5 Sudoterb (Pyrrole, LL-4858)
    12. 3.2.6 Peptideformylase Inhibitor BB-3497
    13. 3.2.7 Phenothiazines
    14. 3.3 Conclusions
  • Chapter 4 Drug Resistance in Mycobacterium Tuberculosis

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    1. 4.1 Major Mechanisms Involved in Thedevelopment of Drug Resistance in Microorganisms
    2. 4.1.1 Drug - Resistant Tuberculosis
    3. 4.1.2 Multi-Drug Resistant Tuberculosis (MDR-TB)
    4. 4.1.3 Extensive-Drug Resistant Tuberculosis (XDR-TB)
    5. 4.1.4 Basic Concepts in the Development of Drug-Resistant TB
    6. 4.2 Molecular Basis of Drug Action and Resistance
    7. 4.2.1 Isoniazid (INH)
    8. 4.2.2 Rifampicin (RMP)
    9. 4.2.3 Pyrazinamide (PZA)
    10. 4.2.4 Ethambutol (EMB)
    11. 4.2.5 Aminoglycosides (Streptomycin (SM)/Kanamycin (KM)/Amikacin (AMK)/Capreomycin CPM)
    12. 4.2.6 Fluoroquinolones (FQ)
    13. 4.2.7 Ethionamide (ETH)/Prothionamide (PTH) and Thioamides
    14. 4.2.8 Oxazolidinones
    15. 4.2.9 Cycloserine
    16. 4.3 New Drugs, New Targets and New Resistance Mechanisms
    17. 4.3.1 Nitroimidazoles
    18. 4.3.2 SQ109
    19. 4.3.3 Bedaquiline (TMC207, R207910, Sirturo®)
    20. 4.3.4 Benzothiazinones
    21. 4.4 Conclusions
  • Chapter 5 Strategies for Anti-Tubercular Drug Development

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    1. 5.1 Cell Wall Components Synthesis and Assemblage
    2. 5.1.1 Biosynthesis of Mycolic Acids and Other Lipids
    3. 5.1.2 Mycobacteria Possessing FAS-I and FAS-II Enzymes
    4. 5.2 Targets in Mycolic Acid Biosynthesis
    5. 5.2.1 INH A and Maba
    6. 5.2.2 Kas A and Kas B
    7. 5.2.3 Β-Ketoacyl-ACP Synthaseinhibitors
    8. 5.2.4 FadD32 – AccD4 System
    9. 5.2.5 Methyltransferases
    10. 5.2.6 Polyketide Synthase System (Pks)
    11. 5.2.7 Mmpl3 Transporter Protein
    12. 5.2.8 Biosynthesis of Mycolyl-Arabinogalactan-Peptidoglycan Complex
    13. 5.3 Drug Targets for Tuberculosis
    14. 5.3.1 Peptidoglycan Biosynthesis
    15. 5.3.2 Protein Synthesis as a Target
    16. 5.3.3 Decaprene Biosynthesis
    17. 5.3.4 The MEP Pathway as a Drug Target
    18. 5.4 Enzymes Involved in Amino Acids or Co-Factor Biosynthesis
    19. 5.4.1 Pantothenatesynthetase
    20. 5.4.2 Quinolinatephosphoribosyltransferase (QAPRTase)
    21. 5.4.3 Shikimate Kinase (SK)
    22. 5.4.4 Thymidylate Kinase
    23. 5.5 Targets in DNA Biosynthesis and Metabolism
    24. 5.5.1 Ribonucleotide Reductases
    25. 5.5.2 DNA Ligase
    26. 5.5.3 DNA Topoisomerase
    27. 5.5.4 Respiratory Chain Inhibitors
    28. 5.6 Miscellaneous Targets
    29. 5.6.1 Isocitratelyase (ICL)
    30. 5.6.2 Mycobacterium Protein Tyrosine Phosphatase B (mPTPB)
    31. 5.6.3 Carbonic Anhydrase
    32. 5.6.4 Mycobacterial Thioredoxin Reductase (MtTrxR)
    33. 5.6.5 Glutamine Synthetase (GS)
    34. 5.6.6 Cysteine Biosynthetic Pathway
    35. 5.6.7 Acetohydroxyacid Synthase (AHAS)
    36. 5.7 Conclusions
  • BackMatter

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