Thrombin inhibitors based on [5,5] trans-fused indane lactams

Bioorganic and Medicinal Chemistry Letters

Volumn 9, Issue 12, 1999, Pages 1657-1662

  Pass, Martin ^a   Abu Rabie, Said ^a   Baxter, Andrew ^a   Conroy, Richard ^a   Coote, Steven J ^a   Craven, Andrew P ^a   Finch, Harry ^a   Hindley, Seán ^a   Kelly, Henry A ^a   Lowdon, Andrew W ^a   McDonald, Edward ^a   Mitchell, William L ^a   Pegg, Neil A ^a   Procopiou, Pan A ^a   Ramsden, Nigel G ^a   Thomas, Rhian ^a   Walker, Dawn A ^a   Watson, Nigel S ^a   Jhoti, Harren ^a   Mooney, Christopher J ^a   Tang, Chi Man ^a   Thomas, Pamela J ^a   Parry, Simon ^a   Patel, Champa ^a   more..

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

INDAN DERIVATIVE; LACTAM; THROMBIN INHIBITOR;

ACYLATION; ANTICOAGULATION; ARTICLE; CHEMICAL REACTION; DRUG ACTIVITY; DRUG HYDROLYSIS; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME ACTIVITY;

ANTICOAGULANTS; BINDING SITES; ENZYME INHIBITORS; INDANS; INHIBITORY CONCENTRATION 50; LACTAMS; MODELS, MOLECULAR; STRUCTURE-ACTIVITY RELATIONSHIP; THROMBIN;

EID: 0033591756     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(99)00244-9     Document Type: Article

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18. For convenience we have retained the indane numbering system throughout.
19. Crystals of thrombin/hirugen were soaked overnight with excess compound 18. X-ray data were collected to 2.5Å and the structure refined to an R-factor of 19%.