Developments of indoles as anti-HIV-1 inhibitors.

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.
AuthorsHui Xu, Min Lv
JournalCurrent pharmaceutical design (Curr Pharm Des) Vol. 15 Issue 18 Pg. 2120-48 ( 2009) ISSN: 1873-4286 [Electronic] Netherlands
PMID19519449 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)
Chemical References
  • Anti-HIV Agents
  • CCR5 Receptor Antagonists
  • Indoles
  • Reverse Transcriptase Inhibitors
  • Anti-HIV Agents (adverse effects, chemistry, pharmacology)
  • CCR5 Receptor Antagonists
  • Catalysis (drug effects)
  • Cell Survival (drug effects)
  • HIV-1 (drug effects)
  • Humans
  • Indoles (adverse effects, chemistry, pharmacology, therapeutic use)
  • Molecular Structure
  • Reverse Transcriptase Inhibitors (adverse effects, chemistry, pharmacology)
  • Structure-Activity Relationship

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research network!

Choose Username:
Verify Password:
Type Validation Code Shown: