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Peptide deformylase inhibitors

A Hydroxyl, Alkyl Technology for Novel Antimicrobial Compounds

Inactive Publication Date: 2003-07-23
SMITHKLINE BECKMAN CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

To date, there is no information on the protein expression of mammalian PDF gene homologues or the functional role of this protein (Meinnel T.2000, Parasitology Today, 16(4), 165-168)

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] N-formyl-N-hydroxy-2-(m-biphenoxy)ethylamine,

[0035] 1a. A solution of tert-butyldimethylsiloxyacetaldehyde (500 mg) in pyridine (5 mL) was treated with O-benzylhydroxylamine hydrochloride (551 mg) and stirred for 90 minutes. Dilute with dichloromethane and extract the reaction solution with 1M HCl. The organics were dried and concentrated to give the oxime (784 mg) as a 1:1 mixture of cis and trans isomers as a colorless oil.

[0036] 1c. To a solution of the above oxime (784mg) in methanol (14mL) at 0°C was added methyl orange. Sodium cyanoborohydride (230 mg) was added slowly with stirring along with the dropwise addition of 6M HCl / methanol (1 / 1 ) as needed to maintain the pink color of the methyl orange indicator. After stirring at 0° C. for 1 hour, the reaction solution was adjusted to pH 9 with 6M NaOH, and the reaction solution was extracted with dichloromethane. Drying and concentration of the organics gave the reducing amine (780mg) as a colorless oil.

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PUM

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Abstract

PDF inhibitors and novel methods for their use are provided.

Description

field of invention [0001] The present invention relates to the use of novel antibacterial compounds, as well as pharmaceutical compositions containing these compounds as peptide deformylase inhibitors. Background of the invention [0002] Bacterial elicitor methionyl tRNA can be modified by methionyl tRNA formyltransferase (FMT) to generate formyl-methionyl tRNA. Formylmethionine (f-met) was then incorporated into the N-terminus of the newly synthesized polypeptide. Polypeptide deformylase (PDF or Def) then deformylates the primary transfer product to generate N-methionyl polypeptide. Most intracellular proteins are further processed by methionine aminopeptidase (MAP), producing mature peptides and free methionine, which is recycled. Both PDF and MAP are essential for bacterial growth, and PDF is required for MAP activity. This series of reactions is called the methionine cycle (Figure 1). [0003] Figure 1. The Methionine Cycle [0004] So far, h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P11/00A61K31/16A61K31/165A61P31/04
CPCA61K31/165A61P11/00A61P31/04A61K31/13
Inventor 凯利·M·奥巴特西格弗里德·B·克里斯坦森第四雅克·布赖恩德马克斯韦尔·D·卡明斯
Owner SMITHKLINE BECKMAN CORP
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