title: Small molecule HIV entry inhibitors: Part II. Attachment and fusion inhibitors: 2004-2010.
abstract: BACKGROUND
  The first US FDA approved HIV entry inhibitor drug Enfuvirdine belongs to the fusion inhibitor category. Earlier efforts in this area were focused on peptides and monoclonal antibodies; recently, the focus has shifted towards the development of small molecule HIV attachment and fusion inhibitors. They can be used for prophylactic purposes and also hold potential for the development of HIV microbicides.
  
  
  METHODS
  In a previous paper ('Small molecule HIV entry inhibitors: Part I'), we reviewed patents and patent applications for small molecule chemokine receptor antagonists from major pharmaceutical companies. In this paper, the development of small molecule HIV attachment and fusion inhibitors is discussed in detail. It covers patents and patent applications for small molecule HIV attachment and fusion inhibitors published between 2004 and 2010 and related literature with a focus on recent developments based on lead generation and lead modification.
  
  
  CONCLUSIONS
  To augment the potency of currently available antiretroviral drug combinations and to fight drug-resistant virus variants, more effective drugs which target additional steps in the viral replication cycle are urgently needed. HIV attachment and fusion processes are such targets. Inhibitors of these targets will provide additional options for the treatment of HIV drug-resistant strains. Small molecule HIV attachment inhibitors such as BMS-378806 and analogs from Bristol Myers Squibb, N-aryl piperidine derivatives from Propharmacon, and NBD-556 and NBD-557 from New York Blood Center may have potential as vaginal microbicidal agents and can be an economical alternative to monoclonal antibodies.
authors.affiliation: National Institute of Pharmaceutical Education and Research (NIPER), Department of Natural Products, Sector-67, S.A.S. Nagar, Punjab 160062, India. ipsingh@niper.ac.in
authors.forename: Inder Pal
authors.initials: IP
authors.lastname: Singh
authors.forename: Siddheshwar Kisan
authors.initials: SK
authors.lastname: Chauthe
mesh_terms: D055808:Drug Discovery; D023581:HIV Fusion Inhibitors / Q000494:pharmacology*; D010330:Patents as Topic; D011355:Prodrugs / Q000494:pharmacology; D013997:Time Factors
chemical_list: D023581:HIV Fusion Inhibitors; D011355:Prodrugs