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Structure--activity relationships of the peptide deformylase inhibitor BB-3497: modification of the P2' and P3' side chains.

Abstract：

:Structural modifications to the peptide deformylase inhibitor BB-3497 are described. In this paper, we describe the initial SAR around this lead for modifications to both the P2' and P3' side chains. Enzyme inhibition and antibacterial activity data revealed that a variety of substituents are tolerated at the P2' and P3' positions of the inhibitor backbone. The data from this study highlights the potential for modification at the P2' and P3' positions to optimise the physicochemical properties.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Davies SJ,Ayscough AP,Beckett RP,Clements JM,Doel S,Pratt LM,Spavold ZM,Thomas SW,Whittaker M

doi

10.1016/s0960-894x(03)00533-x

subject

Has Abstract

pub_date

2003-08-18 00:00:00

pages

2715-8

issue

16

eissn

0960-894X

issn

1464-3405

pii

S0960894X0300533X

journal_volume

13

pub_type

杂志文章

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