Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa |
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| Authors: | Hanessian Stephen Larsson Andreas Fex Tomas Knecht Wolfgang Blomberg Niklas |
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| Affiliation: | Department of Chemistry, Université de Montréal, Montréal, QC, Canada. stephen.hanessian@umontreal.ca |
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| 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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