Matches in SemOpenAlex for { <https://semopenalex.org/work/W2950897182> ?p ?o ?g. }
Showing items 1 to 74 of
74
with 100 items per page.
- W2950897182 endingPage "1075" @default.
- W2950897182 startingPage "1043" @default.
- W2950897182 abstract "Thrombin plays a key role in the control of thrombus formation, for which reason its inhibition has become a target for new antithrombotics. Important issues in the profile of the ideal thrombin inhibitor are: potency, selectivity, oral bioavailability, half-life in the circulatory system and safety. Although many potent direct inhibitors of thrombin have been discovered, most of these inhibitors lack sufficient oral bioavailability. This is often associated with the presence of highly basic functionalities such as guanidine or amidine. These basic functionalities in the P1 moiety are preferred by thrombin and are present in the first generation of thrombin inhibitors. Recently, several orally active direct thrombin inhibitors have been disclosed. Most of these inhibitors originate from leads of the first generation. Two major optimization strategies could be identified to further improve these leads: A: maintain the highly basic P1 moiety and compensate its negative effects, and B: reduce the basicity of the Pi moiety and compensate for the decrease in inhibitory activity. The progress made using these strategies is evaluated. In addition, screening large sets of compounds yielded new structures that provide useful starting points for optimization. The optimization strategy used to convert leads from screening into potent orally active thrombin inhibitors is also be evaluated." @default.
- W2950897182 created "2019-06-27" @default.
- W2950897182 creator A5032085791 @default.
- W2950897182 creator A5037404053 @default.
- W2950897182 date "1999-12-01" @default.
- W2950897182 modified "2023-10-14" @default.
- W2950897182 title "Strategies and Progress Towards the Ideal Orally Active Thrombin Inhibitor" @default.
- W2950897182 doi "https://doi.org/10.2174/1381612805666230112212954" @default.
- W2950897182 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/10607861" @default.
- W2950897182 hasPublicationYear "1999" @default.
- W2950897182 type Work @default.
- W2950897182 sameAs 2950897182 @default.
- W2950897182 citedByCount "50" @default.
- W2950897182 countsByYear W29508971822012 @default.
- W2950897182 countsByYear W29508971822013 @default.
- W2950897182 countsByYear W29508971822014 @default.
- W2950897182 countsByYear W29508971822016 @default.
- W2950897182 crossrefType "journal-article" @default.
- W2950897182 hasAuthorship W2950897182A5032085791 @default.
- W2950897182 hasAuthorship W2950897182A5037404053 @default.
- W2950897182 hasConcept C181389837 @default.
- W2950897182 hasConcept C185592680 @default.
- W2950897182 hasConcept C202751555 @default.
- W2950897182 hasConcept C203014093 @default.
- W2950897182 hasConcept C21951064 @default.
- W2950897182 hasConcept C2776568683 @default.
- W2950897182 hasConcept C2777292125 @default.
- W2950897182 hasConcept C2778622868 @default.
- W2950897182 hasConcept C2779463914 @default.
- W2950897182 hasConcept C3017990168 @default.
- W2950897182 hasConcept C55493867 @default.
- W2950897182 hasConcept C57002609 @default.
- W2950897182 hasConcept C71240020 @default.
- W2950897182 hasConcept C71924100 @default.
- W2950897182 hasConcept C89560881 @default.
- W2950897182 hasConcept C98274493 @default.
- W2950897182 hasConceptScore W2950897182C181389837 @default.
- W2950897182 hasConceptScore W2950897182C185592680 @default.
- W2950897182 hasConceptScore W2950897182C202751555 @default.
- W2950897182 hasConceptScore W2950897182C203014093 @default.
- W2950897182 hasConceptScore W2950897182C21951064 @default.
- W2950897182 hasConceptScore W2950897182C2776568683 @default.
- W2950897182 hasConceptScore W2950897182C2777292125 @default.
- W2950897182 hasConceptScore W2950897182C2778622868 @default.
- W2950897182 hasConceptScore W2950897182C2779463914 @default.
- W2950897182 hasConceptScore W2950897182C3017990168 @default.
- W2950897182 hasConceptScore W2950897182C55493867 @default.
- W2950897182 hasConceptScore W2950897182C57002609 @default.
- W2950897182 hasConceptScore W2950897182C71240020 @default.
- W2950897182 hasConceptScore W2950897182C71924100 @default.
- W2950897182 hasConceptScore W2950897182C89560881 @default.
- W2950897182 hasConceptScore W2950897182C98274493 @default.
- W2950897182 hasIssue "12" @default.
- W2950897182 hasLocation W29508971821 @default.
- W2950897182 hasLocation W29508971822 @default.
- W2950897182 hasOpenAccess W2950897182 @default.
- W2950897182 hasPrimaryLocation W29508971821 @default.
- W2950897182 hasRelatedWork W1976850996 @default.
- W2950897182 hasRelatedWork W1983815293 @default.
- W2950897182 hasRelatedWork W2008470447 @default.
- W2950897182 hasRelatedWork W2017051291 @default.
- W2950897182 hasRelatedWork W2038758540 @default.
- W2950897182 hasRelatedWork W2040289040 @default.
- W2950897182 hasRelatedWork W2071039014 @default.
- W2950897182 hasRelatedWork W2154323821 @default.
- W2950897182 hasRelatedWork W2950897182 @default.
- W2950897182 hasRelatedWork W2953295853 @default.
- W2950897182 hasVolume "5" @default.
- W2950897182 isParatext "false" @default.
- W2950897182 isRetracted "false" @default.
- W2950897182 magId "2950897182" @default.
- W2950897182 workType "article" @default.