title: Adenosine A(2A) Receptor Antagonists and Parkinson's Disease.
abstract: This Review summarizes and updates the work on adenosine A(2A) receptor antagonists for Parkinson's disease from 2006 to the present. There have been numerous publications, patent applications, and press releases within this time frame that highlight new medicinal chemistry approaches to this attractive and promising target to treat Parkinson's disease. The Review is broken down by scaffold type and will discuss the efforts to optimize particular scaffolds for activity, pharmacokinetics, and other drug discovery parameters. The majority of approaches focus on preparing selective A(2A) antagonists, but a few approaches to dual A(2A)/A(1) antagonists will also be highlighted. The in vivo profiles of compounds will be highlighted and discussed to compare activities across different chemical series. A clinical report and update will be given on compounds that have entered clinical trials.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C. , Welsh and McKean Roads, P.O. Box 776, Spring House, Pennsylvania 19477, United States. bshook@its.jnj.com
authors.forename: Brian C
authors.initials: BC
authors.lastname: Shook
authors.forename: Paul F
authors.initials: PF
authors.lastname: Jackson
mesh_terms: D058917:Adenosine A2 Receptor Antagonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000978:Antiparkinson Agents; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000737:chemistry / Q000494:pharmacology; D006571:Heterocyclic Compounds / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D010300:Parkinson Disease / Q000188:drug therapy*; D043705:Receptor, Adenosine A2A / Q000187:drug effects*; D014970:Xanthines / Q000737:chemistry / Q000494:pharmacology
chemical_list: D058917:Adenosine A2 Receptor Antagonists; D000978:Antiparkinson Agents; D019086:Bridged Bicyclo Compounds, Heterocyclic; D006571:Heterocyclic Compounds; D043705:Receptor, Adenosine A2A; D014970:Xanthines