title: Pyrrolidine-5,5-trans-lactams as novel mechanism-based inhibitors of human cytomegalovirus protease. Part 3: potency and plasma stability.
abstract: Mechanism-based inhibitors of HCMV protease, which are stable to human plasma (> or = 20 h) and have single-figure potency in the microM range against HCMV protease, have been developed based on the dansylproline alpha-methyl pyrrolidine-5,5-trans-lactam nucleus.
authors.affiliation: Department of Medicinal Chemistry CVU UK, GlaxoSmithKline Research and Development, Medicines Research Centre, Gunnels Wood Road, Stevenage, Herts SG1 2NY, UK. adb3028@glaxowellcome.co.uk
authors.forename: Alan D
authors.initials: AD
authors.lastname: Borthwick
authors.forename: Anne M
authors.initials: AM
authors.lastname: Exall
authors.forename: Terry M
authors.initials: TM
authors.lastname: Haley
authors.forename: Deborah L
authors.initials: DL
authors.lastname: Jackson
authors.forename: Andrew M
authors.initials: AM
authors.lastname: Mason
authors.forename: Gordon G
authors.initials: GG
authors.lastname: Weingarten
mesh_terms: D000998:Antiviral Agents / Q000737:chemistry* / Q000494:pharmacology*; D003587:Cytomegalovirus / Q000201:enzymology*; D003619:Dansyl Compounds / Q000737:chemistry; D004355:Drug Stability; D006207:Half-Life; D006801:Humans; D020128:Inhibitory Concentration 50; D007769:Lactams / Q000097:blood / Q000737:chemistry / Q000494:pharmacology*; D011392:Proline / Q000031:analogs & derivatives* / Q000737:chemistry; D011480:Protease Inhibitors / Q000097:blood / Q000737:chemistry* / Q000494:pharmacology*; D011759:Pyrrolidines / Q000097:blood / Q000737:chemistry* / Q000494:pharmacology*; D021241:Spectrometry, Mass, Electrospray Ionization
chemical_list: D000998:Antiviral Agents; D003619:Dansyl Compounds; D007769:Lactams; D011480:Protease Inhibitors; D011759:Pyrrolidines; C086697:dansylproline; D011392:Proline