title: Guanylpiperidine peptidomimetics: potent and selective bis-cation inhibitors of factor Xa.
abstract: A novel series of rigid P3-guanylpiperidine peptide mimics 3-14 was designed as potential factor Xa and prothrombinase inhibitors. Incorporation into a P2-gly-P1-argininal motif led to highly potent and selective inhibitors. The synthesis and biological activities of these derivatives are reported herein.
authors.affiliation: Corvas International, Inc., Department of Medicinal Chemistry, San Diego, CA 92121, USA.
authors.forename: S Y
authors.initials: SY
authors.lastname: Tamura
authors.forename: O E
authors.initials: OE
authors.lastname: Levy
authors.forename: T H
authors.initials: TH
authors.lastname: Uong
authors.forename: J E
authors.initials: JE
authors.lastname: Reiner
authors.forename: E A
authors.initials: EA
authors.lastname: Goldman
authors.forename: J Z
authors.initials: JZ
authors.lastname: Ho
authors.forename: C R
authors.initials: CR
authors.lastname: Cohen
authors.forename: P W
authors.initials: PW
authors.lastname: Bergum
authors.forename: R F
authors.initials: RF
authors.lastname: Nutt
authors.forename: T K
authors.initials: TK
authors.lastname: Brunck
authors.forename: J E
authors.initials: JE
authors.lastname: Semple
mesh_terms: D002412:Cations; D065427:Factor Xa Inhibitors; D006147:Guanine / Q000031:analogs & derivatives / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D018716:Molecular Mimicry; D010455:Peptides / Q000737:chemistry*; D010880:Piperidines / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D015842:Serine Proteinase Inhibitors / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D002412:Cations; D065427:Factor Xa Inhibitors; D010455:Peptides; D010880:Piperidines; D015842:Serine Proteinase Inhibitors; D006147:Guanine