title: Investigation of the S3 site of thrombin: design, synthesis and biological activity of 4-substituted 3-amino-2-pyridones incorporating P1-argininals.
abstract: A novel scaffold for P4-P2 dipeptide mimics containing a rigid pyridone spacer was designed based on a virtual library strategy. Several selected nonpeptidic 4-aralkyl or 4-alkylpyridones incorporating a P1-argininal sequence were prepared. The modeling studies, synthesis and biological activities of these unique pyridone derivatives are reported herein.
authors: Corvas International, Inc., Department of Medicinal Chemistry, San Diego, California 92121, USA.
authors: J E
authors: JE
authors: Reiner
authors: M S
authors: MS
authors: Lim-Wilby
authors: T K
authors: TK
authors: Brunck
authors: T
authors: T
authors: Ha-Uong
authors: E A
authors: EA
authors: Goldman
authors: M A
authors: MA
authors: Abelman
authors: R F
authors: RF
authors: Nutt
authors: J E
authors: JE
authors: Semple
authors: S Y
authors: SY
authors: Tamura
mesh_terms: D001120:Arginine / Q000737:chemistry*; D015951:Factor Xa / Q000494:pharmacology; D005341:Fibrinolysin / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008956:Models, Chemical; D011728:Pyridones / Q000138:chemical synthesis*; D013917:Thrombin / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D014357:Trypsin / Q000494:pharmacology
chemical_list: D011728:Pyridones; D001120:Arginine; D014357:Trypsin; D013917:Thrombin; D015951:Factor Xa; D005341:Fibrinolysin