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Non-covalent thrombin inhibitors featuring P3-heterocycles with P1-bicyclic arginine surrogates.
Cui, Jingrong Jean; Araldi, Gian-Luca; Reiner, John E; Reddy, Komandla Malla; Kemp, Scott J; Ho, Jonathan Z; Siev, Daniel V; Mamedova, Lala; Gibson, Tony S; Gaudette, John A; Minami, Nathaniel K; Anderson, Susanne M; Bradbury, Annette E; Nolan, Thomas G; Semple, J Edward.
Affiliation
  • Cui JJ; Department of Medicinal Chemistry, Corvas International, Inc., 3030 Science Park Road, San Diego, CA 92121, USA.
Bioorg Med Chem Lett ; 12(20): 2925-30, 2002 Oct 21.
Article in En | MEDLINE | ID: mdl-12270176
ABSTRACT
Novel, potent, and highly selective classes of thrombin inhibitors were identified, which resulted from judicious combination of P4-aromatics and P2-P3-heterocyclic dipeptide surrogates with weakly basic (calcd pKa approximately non-basic-8.6) bicyclic P1-arginine mimics. The design, synthesis, and biological activity of achiral, non-covalent, orally bioavailable inhibitors NC1-NC44 featuring P1-indazoles, benzimidazoles, indoles, benzotriazoles, and aminobenzisoxazoles is disclosed.
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Collection: 01-internacional Database: MEDLINE Main subject: Bridged Bicyclo Compounds / Thrombin / Enzyme Inhibitors / Heterocyclic Compounds, 3-Ring Type of study: Prognostic_studies Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2002 Document type: Article Affiliation country: United States
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Collection: 01-internacional Database: MEDLINE Main subject: Bridged Bicyclo Compounds / Thrombin / Enzyme Inhibitors / Heterocyclic Compounds, 3-Ring Type of study: Prognostic_studies Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2002 Document type: Article Affiliation country: United States