title: Identification of a 3-aminoimidazo[1,2-a]pyridine inhibitor of HIV-1 reverse transcriptase.
abstract: BACKGROUND
  Despite the effectiveness of highly active antiretroviral therapy (HAART), there remains an urgent need to develop new human immunodeficiency virus type 1 (HIV-1) inhibitors with better pharmacokinetic properties that are well tolerated, and that block common drug resistant virus strains.
  
  
  METHODS
  Here we screened an in-house small molecule library for novel inhibitors of HIV-1 replication.
  
  
  RESULTS
  An active compound containing a 3-aminoimidazo[1,2-a]pyridine scaffold was identified and quantitatively characterized as a non-nucleoside reverse transcriptase inhibitor (NNRTI).
  
  
  CONCLUSIONS
  The potency of this compound coupled with its inexpensive chemical synthesis and tractability for downstream SAR analysis make this inhibitor a suitable lead candidate for further development as an antiviral drug.
authors.affiliation: The Salk Institute for Biological Studies, Nomis Center for Immunobiology and Microbial Pathogenesis, 10010 North Torrey Pines Road, La Jolla, CA 92037, USA.
authors.forename: Daniel
authors.initials: D
authors.lastname: Elleder
authors.forename: Thomas J
authors.initials: TJ
authors.lastname: Baiga
authors.forename: Rebecca L
authors.initials: RL
authors.lastname: Russell
authors.forename: John A
authors.initials: JA
authors.lastname: Naughton
authors.forename: Stephen H
authors.initials: SH
authors.lastname: Hughes
authors.forename: Joseph P
authors.initials: JP
authors.lastname: Noel
authors.forename: John A T
authors.initials: JA
authors.lastname: Young
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D015658:HIV Infections / Q000188:drug therapy / Q000821:virology*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology / Q000502:physiology; D006801:Humans; D007093:Imidazoles / Q000737:chemistry / Q000494:pharmacology*; D011719:Pyrazines / Q000737:chemistry / Q000494:pharmacology*; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D054852:Small Molecule Libraries / Q000494:pharmacology
chemical_list: C579748:3-aminoimidazo(1,2-a)pyrazine; D019380:Anti-HIV Agents; D007093:Imidazoles; D011719:Pyrazines; D018894:Reverse Transcriptase Inhibitors; D054852:Small Molecule Libraries; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase