Chemical biology & drug design, 2008-09, Vol.72 (3), p.189-196
2008
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Details
- Autor(en) / Beteiligte
- Titel
- Reversible and Competitive Cinnamoyl Triazole Inhibitors of Tissue Transglutaminase
- Ist Teil von
- Chemical biology & drug design, 2008-09, Vol.72 (3), p.189-196
- Ort / Verlag
- Oxford, UK: Oxford, UK : Blackwell Publishing Ltd
- Erscheinungsjahr
- 2008
- Quelle
- Wiley Online Library - AutoHoldings Journals
- Beschreibungen/Notizen
- A series of 15 cinnamoyl triazole derivatives was prepared by Cu(I)-catalyzed azide/alkyne [3+2]-cycloaddition reactions and examined as inhibitors of guinea-pig liver transglutaminase. Several compounds exhibited activity as reversible inhibitors that were competitive with acyl donor transglutaminase substrates. For example, triazole 4d has a Ki value of 174 n m and represents one of the most potent reversible transglutaminase inhibitors reported to date.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 1747-0277eISSN: 1747-0285DOI: 10.1111/j.1747-0285.2008.00696.xTitel-ID: cdi_proquest_miscellaneous_69650739
- Format
- –
- Schlagworte
- Alkynes - chemistry, Animals, Azides - chemistry, Catalysis, Cinnamates - chemistry, Cinnamates - pharmacology, cinnamoyl, cycloaddition, enzyme inhibition, Enzyme Inhibitors - chemical synthesis, Enzyme Inhibitors - chemistry, Enzyme Inhibitors - pharmacology, GTP-Binding Proteins - antagonists & inhibitors, GTP-Binding Proteins - metabolism, Guinea Pigs, heterocycle, transglutaminase, Transglutaminases - antagonists & inhibitors, Transglutaminases - metabolism, triazole, Triazoles - chemical synthesis, Triazoles - chemistry, Triazoles - pharmacology