An interview with the Chair of the ACS MEDI division. Interview by Peter Robins

Following the conclusion of the 215th National Meeting of the American Chemical Society Meeting in Dallas, Current Drugs Editor, Peter Robins, spoke to the Chair of the ACS Division of Medicinal Chemistry, Annette Doherty, of Parke-Davis/ Jouveinal in Fresnes, France.     

N15-alkyl and N15,N15-dialkyl derivatives of teicoplanin antibiotics

The synthesis and the biological properties of a series of N15-alkyl and N15,N15-dialkyl derivatives of teicoplanin A2, its pseudoaglycones and aglycone are described. The alkylation of the terminal amino group did not affect the ability of these teicoplanin derivatives to bind with Ac2-L-Lys-D-Ala-D-Ala, a synthetic model of the antibiotic's target peptide in bacterial cell walls, but influenced their in vitro and in vivo antimicrobial activities to a different extent, depending on the structure and length of the alkyl chains and the type and number of sugars present.     

—N,N‘—二（间二甲胺基苯基）—3,6—二甲基—1,4二氢 …

由３,６－二甲基－１,６二氢－１２,４,５－四嗪、双光气和间－（Ｎ,Ｎ－二甲胺基）苯胺反应生成的新化合物Ｎ,Ｎ’－二（间二甲胺基苯基）－３,６－二甲基－１,４－二氢－１,２,４,５－四嗪－１,４－二甲酰胺对Ｐ３８８和Ａ－５４９肿瘤细胞的生长具有明显的抑制作用。同时分离得到未见文献报道的副产物Ｎ,Ｎ’－二（间二甲胺基）苯基脲。