Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa
(2010) In Bioorganic & Medicinal Chemistry Letters 20(23). p.6925-6928- Abstract
The synthesis of a series of novel macrocyclic compounds designed to target blood coagulation Factor XIa is described. The compounds were evaluated for their inhibition of a small set of serine proteases. Several compounds displayed modest activity and good selectivity for Factor XIa. Within the series, a promising lead structure for developing novel macrocyclic inhibitors of thrombin was identified.
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https://lup.lub.lu.se/record/ab15cb86-d84e-473d-a604-5173c5af71cf
- author
- Hanessian, Stephen ; Larsson, Andreas ; Fex, Tomas ; Knecht, Wolfgang LU and Blomberg, Niklas
- publishing date
- 2010-12-01
- type
- Contribution to journal
- publication status
- published
- keywords
- Anticoagulants/chemical synthesis, Blood Coagulation/drug effects, Drug Design, Factor XIa/antagonists & inhibitors, Indoles/chemistry, Serine Proteinase Inhibitors/chemistry, Structure-Activity Relationship
- in
- Bioorganic & Medicinal Chemistry Letters
- volume
- 20
- issue
- 23
- pages
- 6925 - 6928
- publisher
- Elsevier
- external identifiers
-
- scopus:78149280530
- pmid:21035339
- ISSN
- 0960-894X
- DOI
- 10.1016/j.bmcl.2010.09.141
- language
- English
- LU publication?
- no
- id
- ab15cb86-d84e-473d-a604-5173c5af71cf
- date added to LUP
- 2020-07-17 14:17:11
- date last changed
- 2024-07-10 20:26:42
@article{ab15cb86-d84e-473d-a604-5173c5af71cf, abstract = {{<p>The synthesis of a series of novel macrocyclic compounds designed to target blood coagulation Factor XIa is described. The compounds were evaluated for their inhibition of a small set of serine proteases. Several compounds displayed modest activity and good selectivity for Factor XIa. Within the series, a promising lead structure for developing novel macrocyclic inhibitors of thrombin was identified.</p>}}, author = {{Hanessian, Stephen and Larsson, Andreas and Fex, Tomas and Knecht, Wolfgang and Blomberg, Niklas}}, issn = {{0960-894X}}, keywords = {{Anticoagulants/chemical synthesis; Blood Coagulation/drug effects; Drug Design; Factor XIa/antagonists & inhibitors; Indoles/chemistry; Serine Proteinase Inhibitors/chemistry; Structure-Activity Relationship}}, language = {{eng}}, month = {{12}}, number = {{23}}, pages = {{6925--6928}}, publisher = {{Elsevier}}, series = {{Bioorganic & Medicinal Chemistry Letters}}, title = {{Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa}}, url = {{http://dx.doi.org/10.1016/j.bmcl.2010.09.141}}, doi = {{10.1016/j.bmcl.2010.09.141}}, volume = {{20}}, year = {{2010}}, }