167844-89-5Relevant academic research and scientific papers
Cladinose analogues of sixteen-membered macrolide antibiotics. VI. Synthesis of metabolically programmed, highly potent analogues of sixteen-membered macrolide antibiotics
Kurihara, Ken-Ichi,Ajito, Keiichi,Shibahara, Seiji,Hara, Osamu,Araake, Minako,Omoto, Shoji,Inouye, Shigeharu
, p. 771 - 785 (1998)
Five novel 3-hydroxyl derivatives of sixteen-membered macrolide possessing 4-O-acyl-α-L-cladinose as a neutral sugar moiety were synthesized by using a combination of structurally stable silyl acetal protection and selective hydrogenolysis of a 3'-methylthiomethyl ether to a 3'-OMe group. Several derivatives having n-butyryl, i-butyryl and n-valeryl substituent at the 4'-OH group exhibited significant antibacterial activity in vitro. One of them, 4'-O-n-butyryl-3'-O-methylleucomycin V, showed improved therapeutic effect in mice.
