Fine tuning of physico-chemical parameters to optimise a new series of novobiocin analogues

被引:27
|
作者
Schio, L
Chatreaux, F
Loyau, V
Murer, M
Ferreira, A
Mauvais, P
Bonnefoy, A
Klich, M
机构
[1] Aventis Pharma, Med Chem, F-93235 Romainville, France
[2] Aventis Pharma, Struct Anal, F-93235 Romainville, France
[3] Aventis Pharma, Infect Dis, F-93235 Romainville, France
关键词
D O I
10.1016/S0960-894X(01)00257-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A novel series of novobiocin analogues has been synthesised by removing the lipophilic aryl chain in novobiocin and introducing an amino substituent. The structural modifications have been dictated by the control of lipophilicity and the dissociation constant of the resulting compounds. Antibacterial activity of the new coumarin derivatives could be correlated with the amount of uncharged form in physiological conditions. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1461 / 1464
页数:4
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