Immunostimulant and vaccine adjuvant tetra- and penta:peptide(s) - contg. fatty acid acyl gps. e.g. N-alpha-N,N-lauroyl-L-alanyl gamma-D-glutamyl N-epsilon-glycyl-L-lysine

摘要

Tetra- and penta-peptides, based on the parent applicn. 79.16845, having formula (II) and their salts are new R-NH-CH(CH3)-CO-NH-CH(-CO-R1) -CH2-CH2-CO-NH-CHR2-(CH2)3- CHR4-NH-R3 (II) R is H or a fatty acid resdue (pref. 1-45C alkanoyl (opt. substd. by hydroxy, phenyl or cyclohexyl), 3-30C alkenoyl opt. contg. further double bonds or a mycolic acid residue); R1 is hydroxy, amino or 1-4C alkoxy, opt. substd. by phenyl or nitrophenyl; one of R2 and R4 is H, carboxy, carbamoyl, 2-5C alkoxycarbonyl (opt. substd. by phenyl or nitrophenyl), n-carbonyl-glycyl or N-carbonyl-alaryl (opt. esterified by 1-4C alkyl, opt. substd. by phenyl or nitrophenyl) and the other is H, carboxy, carbamoyl or 2-5C alkoxycarbony, (opt. substd. by phenyl or nitrophenyl); R3 is H, a fatty acid residue or glycyl or D-alonyl with the amino gp. substd. by a fatty acid . (II) are immunostimulants and adjuvants (vaccines) which increase hypersensitivity reactions and/or increase prods. of circulating antibodies w.r.t. antigens with which they are admin.. They stimulate, non-specifically, the defince mechanisms against certain infections and tumours, e.g. histeria monocytogenes intracellular bacterial infections in mice. Activity tests are mentioned.