title: Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.
abstract: Amidino-phenoxy quinoline derivatives represent a new class of potent thrombin inhibitors with good selectivity and remarkably low molecular weight (M(W): 335-391). X-ray analyses of thrombin-bound inhibitors revealed that enzyme inhibition is mainly based on hydrophobic interactions.
authors.affiliation: Department of Chemical Research, Boehringer Ingelheim Pharma KG, Birkendorfer Strasse 65, D-88397, Biberach/Riss, Germany. uwe.ries@bc.boehringer-ingelheim.com
authors.forename: Uwe J
authors.initials: UJ
authors.lastname: Ries
authors.forename: Henning W M
authors.initials: HW
authors.lastname: Priepke
authors.forename: Norbert H
authors.initials: NH
authors.lastname: Hauel
authors.forename: Eric E J
authors.initials: EE
authors.lastname: Haaksma
authors.forename: Jean M
authors.initials: JM
authors.lastname: Stassen
authors.forename: Wolfgang
authors.initials: W
authors.lastname: Wienen
authors.forename: Herbert
authors.initials: H
authors.lastname: Nar
mesh_terms: D000578:Amidines / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D018360:Crystallography, X-Ray; D015195:Drug Design; D005341:Fibrinolysin / Q000037:antagonists & inhibitors; D005343:Fibrinolytic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D008958:Models, Molecular; D008970:Molecular Weight; D010314:Partial Thromboplastin Time; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D013917:Thrombin / Q000037:antagonists & inhibitors*; D014361:Trypsin Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D000578:Amidines; D005343:Fibrinolytic Agents; D006571:Heterocyclic Compounds; D007202:Indicators and Reagents; D011804:Quinolines; D014361:Trypsin Inhibitors; C481394:amidino-phenoxy quinoline; D013917:Thrombin; D005341:Fibrinolysin