69977-56-6Relevant articles and documents
Synthesis, opiate receptor binding and analgesic activity of enkephalin analogues
Pless,Bauer,Cardinaux,et al.
, p. 398 - 411 (1979)
The synthesis and biological testing of analogues of Met-enkephalin, a recently discovered opioid peptide from mammalian brain, are described. Testing involved determination of affinity constants for an opiate receptor site and of analgesic potency in the tail-flick test in mouse. The effects on opioid activity on modifying various parts of the enkephalin molecule are discussed. Tyr-D-Ala-Gly-MePhe-Met(O)-ol1) (FK 33-824), which was highly active in these tests, was subsequently selected for clinical testing. The use of two complementary models - in vitro binding studies and in vivo test for analgesia - for the assessment of biological activity in the evaluation of analogues is explained.
Bifunctional bis(oxazolines) as potential ligands in catalytic asymmetric reactions
Hanessian, Stephen,Jnoff, Eric,Bernstein, Noemy,Simard, Michel
, p. 306 - 313 (2007/10/03)
C2-symmetrical bis(oxazoline) ligands bearing pendant alkylthio ether groups were synthesized, and the structures of Cu complexes were determined by single crystal X-ray diffraction. The potential utility in catalysis was shown in the asymmetric addition of methyllithium to an aromatic aldimine, which resulted in a mixture of products with an enantiomeric excess of 68%.
Palladium-catalysed Asymmetric Allylic Substitution: a Ligand Design Incorporating Steric and Electronic Effects
Allen, Joanne V.,Coote, Steven J.,Dawson, Graham J.,Frost, Christopher G.,Martin, Christopher J.,Williams, Jonathon, M.
, p. 2065 - 2072 (2007/10/02)
Enantiomerically pure ligands containing a 4,5-dihydrooxazole moiety tethered to an auxiliary sulfur or phosphorus donor have been prepared.These ligands have been exploited for palladium-catalysed asymmetric allylic substitution, providing enantioselectivity in the catalytic reaction is discussed in terms of the steric and electronic influences provided by the ligand.
