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Optically active iminocarboxylic acid derivatives
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, (2008/06/13)
The compounds of the formula STR1 wherein R is OH, NH2, lower-alkyl-NH or phenyl-lower alkyl-NH are presented. These compounds can be catalytically hydrogenated to the corresponding α-aminocarboxylic acid derivatives which are intermediates in the synthesis of therapeutic pseudopeptides.
Synthesis, enzymic degradation, lipophilic properties, and biological activity of [D-alanine2, t-butylglycine 5]enkephalin amide
Fauchere,Petermann
, p. 824 - 831 (2007/10/02)
L-C(a)-t-Butylglycine (Bug), its amide, methyl ester, and N(a)-t-butoxycarbonyl derivative were prepared by an asymmetric synthesis, and the Hansch side-chain hydrophobic (lipophilicity) parameter determined. A new enkephalin analogue, H . Tyr-D-Ala-Gly-Phe-Bug . HN2 was synthesized which is pharmacologically active in two in vitro assays and strongly resistant against a number of enzymes in vitro.