title: From natural products to achiral drug prototypes: potent thrombin inhibitors based on P2/P3 dihydropyrid-2-one core motifs.
abstract: A series of dihydropyrid-2-ones was synthesized and tested for inhibitory activity against serine protease enzymes. Moderate to low nanomolar inhibitory activities were obtained against thrombin and excellent selectivity against trypsin was observed.
authors.affiliation: Department of Chemistry, Université de Montréal, C. P. 6128, Succ. Centre-Ville, Montréal, P. Q., Canada H3C 3J7. stephen.hanessian@umontreal.ca
authors.forename: Stephen
authors.initials: S
authors.lastname: Hanessian
authors.forename: Eric
authors.initials: E
authors.lastname: Therrien
authors.forename: Jianbin
authors.initials: J
authors.lastname: Zhang
authors.forename: Willem van
authors.initials: Wv
authors.lastname: Otterlo
authors.forename: Yafeng
authors.initials: Y
authors.lastname: Xue
authors.forename: David
authors.initials: D
authors.lastname: Gustafsson
authors.forename: Ingemar
authors.initials: I
authors.lastname: Nilsson
authors.forename: Ola
authors.initials: O
authors.lastname: Fjellström
mesh_terms: D000818:Animals; D002417:Cattle; D018360:Crystallography, X-Ray; D006801:Humans; D008958:Models, Molecular; D011485:Protein Binding; D011728:Pyridones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013917:Thrombin / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism*; D014357:Trypsin / Q000378:metabolism
chemical_list: D011728:Pyridones; D015842:Serine Proteinase Inhibitors; D014357:Trypsin; D013917:Thrombin