title: Solid phase synthesis of novel pyrrolidinedione analogs as potent HIV-1 integrase inhibitors.
abstract: A novel series of HIV-1 integrase inhibitors were identified from a 100 member (4R(1) x 5R(2) x 5R(3)) library of pyrrolidinedione amides. A solid-phase route was developed which facilitates the simultaneous variation at R(1), R(2), and R(3) of the pyrrolidinedione scaffold. The resulting library samples were assayed for HIV-1 integrase activity and analyzed to determine the R(1), R(2), and R(3) reagent contributions towards the activity.
authors.affiliation: Bristol-Myers Squibb Research and Development, Wallingford, Connecticut 06492, USA. annapurna.pendri@bms.com
authors.forename: Annapurna
authors.initials: A
authors.lastname: Pendri
authors.forename: Timothy L
authors.initials: TL
authors.lastname: Troyer
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Sofia
authors.forename: Michael A
authors.initials: MA
authors.lastname: Walker
authors.forename: B Narasimhulu
authors.initials: BN
authors.lastname: Naidu
authors.forename: Jacques
authors.initials: J
authors.lastname: Banville
authors.forename: Nicholas A
authors.initials: NA
authors.lastname: Meanwell
authors.forename: Ira
authors.initials: I
authors.lastname: Dicker
authors.forename: Zeyu
authors.initials: Z
authors.lastname: Lin
authors.forename: Mark
authors.initials: M
authors.lastname: Krystal
authors.forename: Samuel W
authors.initials: SW
authors.lastname: Gerritz
mesh_terms: D020650:Combinatorial Chemistry Techniques / Q000379:methods; D015195:Drug Design; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D013388:Succinimides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D019428:HIV Integrase Inhibitors; D013388:Succinimides