Anti HIV Drugs. Non-Nucleoside Reverse Transcriptase Inhibitors E-Book

Amit Patel

• Herausgeber: GRIN Verlag
• Sprache: Englisch

Veröffentlichungsjahr: 2014

Beschreibung

Literature Review from the year 2014 in the subject Chemistry - Other, , language: English, abstract: The proposed book entitled, “Anti HIV Drugs: Non-Nucleoside Reverse Transcriptase Inhibitors” gives an outline of the Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI) class of Anti HIV drugs, from the initial discovery of the class in 1990 to the current compounds in clinical development, i.e. around 20 years of research and development efforts. It describes the characteristics of the NNRTIs, their mechanisms of action, HIV resistance to the inhibitors, and the drugs that have been approved for the treatment of HIV infection, that are currently in clinical development. The role of NNRTIs in prevention of HIV transmission is also addressed. The book also covers some basic information about HIV, AIDS and HIV life cycle.

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Preface

The proposed book entitled, “Anti HIV Drugs:Non-Nucleoside Reverse Transcriptase Inhibitors” gives an outlineof the Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTI) class of Anti HIV drugs, from the initial discovery of the class in 1990 to the current compounds in clinical development, i.e. around 20 years of research and development efforts. It describes the characteristics of the NNRTIs, their mechanisms of action, HIV resistance to the inhibitors, and the drugs that have been approved for the treatment of HIV infection, that are currently in clinical development. The role of NNRTIs in prevention of HIV transmission is also addressed. The book also covers some basic information about HIV, AIDS and HIV life cycle.

ACKNOWLEDGEMENTS

This Book would not have been possible without the guidance and the help of several individuals who in one way or another contributed and extended their valuable assistance in the preparation and completion of this study. It is a pleasure to convey my gratitude to them all in my humble acknowledgment.

I convey my heartfelt thanks to Director, Sardar Vallabhbhai National Institute of Technology, Surat for providing me all the required facilities and financial assistance to carry out my research work.

It is a pleasure to express my sincere gratitude to HVHP Institute of Postgraduate Studies and Research and Kadi Sarva Vishwavidyalaya for providing a wonderful working environment. There are no proper words to convey my deep gratitude and respect to Dr. Hasit Dangi, whom I was fortunate to meet when he was holding an honorary Senior Manager’s position at Bayer Crop Science. He has inspired me to become an independent researcher and helped me realize the power of critical reasoning.

A journey is easier when you travel together. Interdependence is certainly more valuable than independence. This book is the result of love from my wife Vibhu, who was always there when I really needed. Thank you doesn’t seem sufficient but it is said with appreciation and respect for her support, encouragement, care, understanding and precious friendship. My son Avi owed a debt of gratitude by me for sacrificing playtime while his father typed away in the basement. This helped me a lot to work for hours together tirelessly.During my research work there was continues support from my family. It was their kindness and patience that they allowed my absence from my family duties. I have no words to express my gratitude for the unconditional love, support, inspiration and blessings given by my father Shri Babubhai F. Mahyavanshi and my mother Smt. Chanchalben B. Mahyavanshi.

Besides this, several people have knowingly and unknowingly helped me in the successful completion of this book. I doubt that I will ever be able to convey my appreciation fully, but I owe such people my eternal gratitude.

Table of Contents

Preface

ACKNOWLEDGEMENTS

List of Figures

List of Tables

List of Abbreviations

1.0. History

2.0. HIV Virus

2.1. Structure of HIV

2.2. HIV Life Cycle: [19, 20]

2.2.1. Entry or Binding and Fusion

2.2.2. Reverse Transcription (RT)

2.2.3. Integration (IN)

2.2.4. Transcription

2.2.5. Assembly

2.2.6. Budding

2.2.7. Maturation

3.0. Anti HIV Drugs

3.1. Classification of Anti HIV Drugs [22]

3.1.1. Entry Inhibitors

3.1.2. Integrase Inhibitors

3.1.3. Nucleoside (NRTI) and Nucleotide (NtRTIs) Reverse Transcriptase Inhibitors

3.1.4. Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)

3.1.5. Protease Inhibitors (PIs)

3.2. FDA approved Anti HIV Drugs: [23]

4.0. Non-Nucleoside Reverse Transcriptase Inhibitors

4.1. HIV Reverse Transcriptase (RT) enzyme: [24]

4.2. Mechanism of action of NNRTIs: [25]

5.0. Important classes of Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)

5.1. TIBO {4,5,6,7-Tetrahydro-5-methylimidazo[4,5,1-jk][1,4]benzodiazepine-2(1H)-ones} derivatives

5.2. HEPT {1-[(2-hydroxyethoxy) methyl]-6-(phenylthio) thymine}

5.3. Pyridinones

5.4. Thiocarboxanilide derivatives

5.5. DABO {Dihydroalkoxybenzyloxopyrimidine}

5.6. DATA {Diaryl triazine}

5.7. DAPYs {Diarylpyrimidines}

5.8. PBOs {Pyrrolobenzoxazepinones}

5.9. Benzoxazinones [43]

5.10. 2- Amino pyrimidine

5.11. Benzophenone

5.12. α-Anilinophenylacetamides (α-APAs)

5.13 Dipyridodiazepinones [43]

5.14 PETT {Phenyl Ethyl Thiourea Thiazole}

5.15. BHAP {Bis (heteroaryl)-Piperazine} derivatives

6.0. HIV and drug resistance

7.0. Highly Active Antiretroviral Therapy

8.0. Conclusion

9.0. References

List of Figures

Figure 1.1 Global prevalence of HIV, 2009

Figure 2.1 Schematic of the HIV virus

Figure-2.2 HIV life cycle

Figure 3.1. Structural formulae of NRTIs and the NtRTI

Figure 3.2 Structural formula of the pyrophosphate analogue foscarnet

Figure 4.1 Mode of action of NNRTIs

Figure 4.2 Diagram comparing the NNRTI site and polymerase active site in Reverse Transcriptase

List of Tables

Table 3.2.1: Fusion Inhibitors

Table 3.2.2: Entry Inhibitors - CCR5 co-receptor antagonist

Table 3.2.3: HIV integrase strand transfer inhibitors

Table 3.2.4: Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

Table 3.2.5: Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)

Table 3.2.6: Protease Inhibitors (PIs)

Table 3.2.7: Multi-class Combination Products

List of Abbreviations