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Synthesis of potent...
Synthesis of potential thrombin inhibitors. Incorporation of tartaric acid templates as P2 proline mimetics
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- Dahlgren, Anders (författare)
- Linköpings universitet,Tekniska högskolan,Organisk Kemi
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- Branalt, J. (författare)
- Brånalt, J., AstraZeneca RandD, Medicinal Chemistry, S-431 83 Mölndal, Sweden
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- Kvarnström, Ingemar (författare)
- Linköpings universitet,Tekniska högskolan,Organisk Kemi
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- Nilsson, I. (författare)
- AstraZeneca RandD, Medicinal Chemistry, S-431 83 Mölndal, Sweden
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- Musil, D. (författare)
- AstraZeneca RandD, Structural Chemistry Laboratory, S-481 83 Mölndal, Sweden
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- Samuelsson, B. (författare)
- Department of Organic Chemistry, Arrhenius Laboratory, Stockholm University, S-106 91 Stockholm, Sweden, Tel.: +46-8-608-3104
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(creator_code:org_t)
- 2002
- 2002
- Engelska.
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Ingår i: Bioorganic & Medicinal Chemistry. - 0968-0896 .- 1464-3391. ; 10:5, s. 1567-1580
- Relaterad länk:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- With the objective to prepare novel non-peptidic thrombin inhibitors, bioisosteres of the inhibitory tripeptide D-Phe-Pro-Arg chain have been examined. Thus, the P1 Arg was replaced with p-amidinobenzylamine, an elongated homologue of the same and with 2,5-dichloro benzylamine. The P2-P3, D-Phe-Pro, was replaced with a novel tartaric acid template coupled to a series of readily available, mainly lipophilic, amines. Some of these compounds exhibit promising thrombin inhibition activity in vitro, IC50~5.9 µM. © 2002 Elsevier Science Ltd. All rights reserved.
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- TECHNOLOGY
- TEKNIKVETENSKAP
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