SYNTHESIS AND ANTIFUNGAL ACTIVITIES OF PRADIMICIN DERIVATIVES, MODIFICATION AT C4'-POSITION

被引：18

作者：

KAMACHI, H

IMURA, S

OKUYAMA, S

HOSHI, H

TAMURA, S

SHINODA, M

SAITOH, K

KONISHI, M

OKI, T

机构：

[1] Bristol-Myers Squibb Research Institute, Bristol-Myers Squibb K.K., Tokyo 153, 2-9-3, Shimo-meguro, Meguro-ku

来源：

JOURNAL OF ANTIBIOTICS | 1992年 / 45卷 / 09期

关键词：

D O I：

10.7164/antibiotics.45.1518

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：

The 4'-N-alkyl(1 approximately 10)and 4'-N-acyl derivatives (11 approximately 21)of pradimicins (PRMs) were synthesized by trimethylsilylation of PRMs A, C and FA-1 followed by condensation with appropriate alkylating and acylating agents. The 4'-hydroxy derivatives (23 and 24) were synthesized from PRM FA-2 in a 3-step sequence. Among these compounds. the 4'-N-carboxylsubstituted alkyl (1, 5, 8 and 10), 4'-N-formyl (11) and 4'-axial-hydroxy (23) derivatives retained the antifungal activity of the parent compounds and showed great improvement in water solubility.

引用

页码：1518 / 1525

页数：8

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