title: Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: selection of the scaffold.
abstract: HIV integrase inhibitors based on a novel bicyclic pyrimidinone core is presented. Nine variations of the core scaffold are evaluated leading to optimization of the 6:6 core giving compound 48 with an EC(50) of 3 nM against wild type HIV infected T-cells.
authors: Avexa Ltd, 576 Swan Street, Richmond, Victoria 3121, Australia.
authors: Eric D
authors: ED
authors: Jones
authors: Nick
authors: N
authors: Vandegraaff
authors: Giang
authors: G
authors: Le
authors: Neil
authors: N
authors: Choi
authors: William
authors: W
authors: Issa
authors: Katherine
authors: K
authors: Macfarlane
authors: Neeranat
authors: N
authors: Thienthong
authors: Lisa J
authors: LJ
authors: Winfield
authors: Jonathan A V
authors: JA
authors: Coates
authors: Long
authors: L
authors: Lu
authors: Xinming
authors: X
authors: Li
authors: Xiao
authors: X
authors: Feng
authors: Changjiang
authors: C
authors: Yu
authors: David I
authors: DI
authors: Rhodes
authors: John J
authors: JJ
authors: Deadman
mesh_terms: D001643:Bridged Bicyclo Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015195:Drug Design; D019427:HIV Integrase / Q000737:chemistry* / Q000378:metabolism; D019428:HIV Integrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013601:T-Lymphocytes / Q000821:virology
chemical_list: D001643:Bridged Bicyclo Compounds; D019428:HIV Integrase Inhibitors; D011725:Pyridines; D011743:Pyrimidines; D019427:HIV Integrase; C514801:p31 integrase protein, Human immunodeficiency virus 1