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2,3,4,5-Tetrahydro-1H-pyrido[2,3-b and e][1,4]diazepines as inhibitors of the bacterial enoyl ACP reductase, FabI.

Abstract：

:In the search for new antibacterial agents, the enzyme FabI has been identified as an attractive target. Employing a structure guided approach, the previously reported ene-amide series of FabI inhibitors were expanded to include 2,3,4,5-tetrahydro-1H-pyrido[2,3-b and e][1,4]diazepines. These novel series incorporate additional H-bonding functions and can be more water soluble than their naphthyridinone progenitors; diazepine 16c is shown to be efficacious in a mouse infection model.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Ramnauth J,Surman MD,Sampson PB,Forrest B,Wilson J,Freeman E,Manning DD,Martin F,Toro A,Domagala M,Awrey DE,Bardouniotis E,Kaplan N,Berman J,Pauls HW

doi

10.1016/j.bmcl.2009.07.094

subject

Has Abstract

pub_date

2009-09-15 00:00:00

pages

5359-62

issue

18

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)01053-1

journal_volume

19

pub_type

杂志文章

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