Journal of Antibiotics p. 771 - 785 (1998)
Update date:2022-08-04
Topics:
Kurihara, Ken-Ichi
Ajito, Keiichi
Shibahara, Seiji
Hara, Osamu
Araake, Minako
Omoto, Shoji
Inouye, Shigeharu
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.
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