Unusually strong lipophilicity of ‘fat’ or ‘super’ amino-acids,including a new reference value for glycine

Summary Lipophilic, steric, electronic, and enzyme resistance characteristics of carboranylalanine, adamantylalanine, neopentylglycine and tert-butylglycine are described. The first 2 amino-acids display lipophilicities 2 orders of magnitude higher than tryptophan.This work was supported by research grants to Prof. R. Schwyzer from the Swiss National Science Foundation.     

Unexpected antibiotic properties of a cephalosporin]

The presence of an oximino group on the methylene of the (2-aminothiazol 4-yl)-acetyl side chain bound to the 7-amino cephalosporanic acid affords derivatives with syn or anti configuration. Whereas the anti isomers display low antibiotic activities, the syn isomers possess a surprising high efficiency against gram negative bacteria, enhanced a factor of 10 to 100 as compared with the cephalosporins known at the moment.