168070-06-2Relevant academic research and scientific papers
Synthesis and evaluation of backbone/amide-modified analogs of leualacin
Hu, Ming-Kuan,Yang, Fu-Chu,Chou, Chi-Cheun,Yen, Mao-Hsiung
, p. 563 - 568 (2007/10/03)
Leualacin (1), a cyclic depsi-pentapeptide, and its backbone/amidemodified analogs 2-4 were synthesized. Amide analogue 3 exhibited stronger vasodilatory effects. It also strongly inhibited collagen- and arachidonic acid (AA)induced platelet aggregations with IC50s of 0.6 μM and 2.0 μM, respectively.
Total synthesis of the cyclic depsipeptide leualacin
McLaren
, p. 6082 - 6084 (2007/10/03)
The fungal metabolite leualacin (1), a potent calcium channel antagonist, was synthesized in 15 steps from commercially available amino acids in 25% overall yield using standard solution methods. The synthesis is general and thus would accommodate the incorporation of amino acid replacements as well as the inclusion of peptide mimics and isosteres.
