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Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa

Hanessian, Stephen ; Larsson, Andreas ; Fex, Tomas ; Knecht, Wolfgang LU and Blomberg, Niklas (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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author
; ; ; and
publishing date
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}},
}