SYNTHESIS AND ANTIFUNGAL ACTIVITY OF PRADIMICIN DERIVATIVES - MODIFICATIONS ON THE AGLYCONE PART

被引:16
作者
ABURAKI, S
OKUYAMA, S
HOSHI, H
KAMACHI, H
NISHIO, M
HASEGAWA, T
MASUYOSHI, S
IIMURA, S
KONISHI, M
OKI, T
机构
[1] Bristol-Myers Squibb Research Institute, Bristol-Myers Squibb K. K., 2-9-3 Shimo-meguro, Meguro-ku
关键词
D O I
10.7164/antibiotics.46.1447
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
Synthesis and antifungal activity of pradimicin analogs modified on the aglycone part is described. Upon modification studies at various sites of the aglycone part using pradimicin A (PRM A), C-11 position was found to be the sole site to be modified without loosing antifungal activity. Further modification studies at C-11 position were carried out with 11-OH derivative of pradimicin T1 (PRM T1) because of its easy availability. Among the compounds prepared, 11-demethoxy derivative of PRM A (12) and 11-O-ethyl (13) and 11-O-fluoroethyl (14) derivatives of PRM T1 showed promising antifungal activity comparable to that of PRM A.
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收藏
页码:1447 / 1457
页数:11
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