| 摘要 |
PCT No. PCT/GB94/02162 Sec. 371 Date Apr. 8, 1996 Sec. 102(e) Date Apr. 8, 1996 PCT Filed Oct. 5, 1994 PCT Pub. No. WO95/09867 PCT Pub. Date Apr. 13, 1995New derivatives of N3-D-trans-2,3-epoxysuccinamoyl-L-2,3-diaminopropanoic acid of formula (1) e residue of an amino acid selected from L-valine, L-norvaline, L-leucine, L-isoleucine, L-norleucine, L-methionine, L-lysine, L-2-aminobutanoic acid, L-aspartic acid and L-glutamic acid; or R1 is the residue of a dipeptide selected from L-norvalyl-L-norvaline, L-lysyl-L-norvaline, L-methionyl-L-norvaline, L-glutamyl-L-norvaline, L-norvalyl-L-methionine, L-methionyl-L-methionine, L-leucyl-L-norvaline, L-norleucyl-L-norvaline, L-valyl-L-norvaline, L-glutamyl-L-leucine, L-asparginyl-L-norvaline and L-leucyl-L-leucine; wherein R2 is hydroxyl; or R2 is the residue of an amino acid selected from L-alanine, L-methionine, L-valine, L-norvaline, L-leucine, L-isoleucine, L-norleucine and L-2-aminobutanoic acid; with the provisos that when R1 is hydrogen then R2 is an amino acid residue and that when R1 is an amino acid residue or a peptide residue then R2 is hydroxyl; the derivative optionally being in the form of a physiologically acceptable salt thereof; are of value as antimicrobial agents, particularly as antifungal agents, especially in relation to Candida albicans. |
