Abstract
Since the first case of acquired immunodeficiency syndrome (AIDS) was reported in 1981, AIDS has always been a global health threat and the leading cause of deaths due to the rapid emergence of drug-resistance and unwanted metabolic side effects. Every day in 2007 an estimated 6850 people were newly infected with human immunodeficiency virus (HIV). Over the past 28 years the rapid worldwide spread of AIDS has prompted an intense research effort to discover compounds that could effectively inhibit HIV. The development of new, selective and safe inhibitors for the treatment of HIV, therefore, still remains a high priority for medical research. To the best of our knowledge, the indole derivatives have been considered as one class of promising HIV-1 inhibitors, such as delavirdine approved by the Food and Drug Administration (FDA) in 1997 for use in combination with other antiretrovirals in adults with HIV infection. In this review we focus on the synthesis and anti-HIV-1 activity of indole derivatives, in the meantime, the structure – activity relationship (SAR) for some derivatives are also surveyed. It will pave the way for the design of indole derivatives as anti- HIV-1 drugs in the future.
Keywords: Indole, synthesis, acquired immunodeficiency syndrome, human immunodeficiency virus, inhibitor, structure, –, activity relationship
Current Pharmaceutical Design
Title: Developments of Indoles as Anti-HIV-1 Inhibitors
Volume: 15 Issue: 18
Author(s): Hui Xu and Min Lv
Affiliation:
Keywords: Indole, synthesis, acquired immunodeficiency syndrome, human immunodeficiency virus, inhibitor, structure, –, activity relationship
Abstract: Since the first case of acquired immunodeficiency syndrome (AIDS) was reported in 1981, AIDS has always been a global health threat and the leading cause of deaths due to the rapid emergence of drug-resistance and unwanted metabolic side effects. Every day in 2007 an estimated 6850 people were newly infected with human immunodeficiency virus (HIV). Over the past 28 years the rapid worldwide spread of AIDS has prompted an intense research effort to discover compounds that could effectively inhibit HIV. The development of new, selective and safe inhibitors for the treatment of HIV, therefore, still remains a high priority for medical research. To the best of our knowledge, the indole derivatives have been considered as one class of promising HIV-1 inhibitors, such as delavirdine approved by the Food and Drug Administration (FDA) in 1997 for use in combination with other antiretrovirals in adults with HIV infection. In this review we focus on the synthesis and anti-HIV-1 activity of indole derivatives, in the meantime, the structure – activity relationship (SAR) for some derivatives are also surveyed. It will pave the way for the design of indole derivatives as anti- HIV-1 drugs in the future.
Export Options
About this article
Cite this article as:
Xu Hui and Lv Min, Developments of Indoles as Anti-HIV-1 Inhibitors, Current Pharmaceutical Design 2009; 15 (18) . https://dx.doi.org/10.2174/138161209788489168
DOI https://dx.doi.org/10.2174/138161209788489168 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...read more
- 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
-
Formulation of Nanosuspensions as a New Approach for the Delivery of Poorly Soluble Drugs
Current Nanoscience Review: Studies on the Synthesis of Quinolone Derivatives with Their Antibacterial Activity (Part 1)
Current Organic Chemistry Oxidative Stress in the Molecular Mechanism of Pathogenesis at Different Diseased States of Organism in Clinics and Experiment
Current Drug Targets - Inflammation & Allergy CRISPeering: Bioengineering the Host Cells through CRISPRCas9 Genome Editing System as the Next-generation of Cell Factories
Recent Patents on Biotechnology Curcumin: Structure-Activity Relationship Towards its Role as a Versatile Multi-Targeted Therapeutics
Mini-Reviews in Organic Chemistry Graphical Abstracts
Medicinal Chemistry Pulmonary Drug Delivery: A Role for Polymeric Nanoparticles?
Current Topics in Medicinal Chemistry The TLR4 ASP299GLY Polymorphism is a Risk Factor for Active Tuberculosis in Caucasian HIV-Infected Patients
Current HIV Research Dichotomous Life of DNA Binding High Mobility Group Box1 Protein in Human Health and Disease
Current Protein & Peptide Science In Vivo Induced Antigen Technology (IVIAT) and Change Mediated Antigen Technology (CMAT)
Infectious Disorders - Drug Targets Vitamin D Intervention Trials in Critical Illness
Inflammation & Allergy - Drug Targets (Discontinued) Harnessing Polypharmacology with Computer-Aided Drug Design and Systems Biology
Current Pharmaceutical Design A New Catalytic Method for Eco-Friendly Synthesis of Quinoxalines by Zirconium (IV) Oxide Chloride Octahydrate Under Mild Conditions
Letters in Organic Chemistry Medicinal Plants as a Source of New Therapeutic Products: Genus Mentha and the Potential Antimicrobial Activity of Extracts and Essential Oils
Current Traditional Medicine Therapeutic Implications of Gene Deletion of Ligands and Receptors of Members of TNF Superfamily
Medicinal Chemistry Reviews - Online (Discontinued) Polymer Particulates in Drug Delivery
Current Pharmaceutical Design Synthesis, ADME Evaluation, and In Vitro Antimycobacterial Studies of a Novel Series of 2-Thiazolylimino-5-Arylidene-4-Thiazolidinone Derivatives
Anti-Infective Agents Host-Pathogen Interactions Made Transparent with the Zebrafish Model
Current Drug Targets Novel Urea/Thiourea Derivatives of Quinazolin-4(3H)-one: Design, Synthesis, Antimicrobial and Anti-TB Study
Letters in Drug Design & Discovery Developing Solid Particulate Vaccine Adjuvants: Surface Bound Antigen Favours a Humoural Response, whereas Entrapped Antigen Shows a Tendency for Cell Mediated Immunity
Current Drug Delivery