658053-32-8Relevant academic research and scientific papers
Suppression of Formation of N,N′-Dicyclohexylurea Derivatives during DCC-Activation of Proline-Containing Dipeptides
Radau, Gregor
, p. 1033 - 1036 (2003)
The syntheses of dipeptide esters containing a C-terminal L-proline moiety using carbodiimides as coupling reagents strongly depend on the choice of appropriate conditions. Thus, the use of DCC prefers the formation of the undesirable N,N′-dicyclohexylurea derivative 3 as a consequence of a CO → N-shift in the O-acyl isourea intermediate instead of the desired dipeptide ester 4. In our hands, only DIC was able to yield the desired product exclusively.
New cyanopeptide-derived low molecular weight thrombin inhibitors
Radau, Gregor,Gebel, Jana,Rauh, Daniel
, p. 372 - 380 (2007/10/03)
Thrombosis is the result of defective regulation of the hemostasis system. This cardiovascular disorder may lead to deep vein thrombosis, myocardial infarction, and stroke. The majority of current drug research is focused on finding inhibitors of thrombin - the global player in hemostasis. In our work, we emphasize investigation of the marine environment to yield new lead structures from marine organisms like blue-green algae (cyanobacteria). This article deals with the design, syntheses, and inhibition tests of new low molecular weight thrombin inhibitors utilizing cyanopeptides, the secondary metabolites of cyanobacteria with interesting biological activities, as new lead structures. Starting with aeruginosin 98-B (2) as a lead structure, we have developed and synthesized new, selective acting inhibitors of thrombin (RA-1001 and RA-1002), which are suitable targets for further structure-activity studies.
