title: Tetrahydrofuran, tetrahydropyran, triazoles and related heterocyclic derivatives as HIV protease inhibitors.
abstract: HIV/AIDS remains a formidable disease with millions of individuals inflicted worldwide. Although treatment regimens have improved considerably, drug resistance brought on by viral mutation continues to erode their effectiveness. Intense research efforts are currently underway in search of new and improved therapies. This review is concerned with the design of novel HIV-1 protease inhibitors that incorporate heterocyclic scaffolds and which have been reported within the recent literature (2005-2010). Various examples in this review showcase the essential role heterocycles play as scaffolds and bioisosteres in HIV-1 protease inhibitor drug development. This review will hopefully stimulate the widespread application of these heterocycles in the design of other therapeutic agents.
authors.affiliation: Department of Chemistry, Purdue University, West Lafayette, Indiana 47907, USA. akghosh@purdue.edu
authors.forename: Arun K
authors.initials: AK
authors.lastname: Ghosh
authors.forename: David D
authors.initials: DD
authors.lastname: Anderson
mesh_terms: D005663:Furans / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D006678:HIV / Q000187:drug effects; D015658:HIV Infections / Q000188:drug therapy*; D017320:HIV Protease Inhibitors / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D006571:Heterocyclic Compounds / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D011714:Pyrans / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D005663:Furans; D017320:HIV Protease Inhibitors; D006571:Heterocyclic Compounds; D011714:Pyrans; D014230:Triazoles; C018674:tetrahydrofuran