234768-83-3

Upstream product

• 143965-32-6 (4S)-3-hexanoyl-4-(phenylmethyl)-1,3-oxazolidin-2-one 
• 29601-98-7 N-benzylhydroxylamine hydrochloride 
• 668485-39-0 (4S)-3-[(2R)-2-(hydroxymethyl)hexanoyl]-4-(phenylmethyl)-1,3-oxazolidin-2-one 
• 142-61-0 Hexanoyl chloride 
• 2985-32-2 butylmalonic acid monoethyl ester 
• 58243-89-3 (±)-2-butyl-3-hydroxypropionic acid 
• 2612-26-2 2-butylpropane-1,3-diol 
• 676127-84-7 (3R)-3-butyl-1-[(phenylmethyl)oxy]-2-azetidinone 
• 676127-83-6 C₁₅H₂₃NO₅S 
• 676127-81-4 (2R)-2-(hydroxymethyl)-N-[(phenylmethyl)oxy]hexanamide 
• 478912-43-5 4-benzyl-3-[2-(benzyloxyamino-methyl)-hexanoyl]-oxazolidin-2-one 
• 234768-82-2 4S-benzyl-3-[2R-(benzyloxyamino-methyl)-hexanoyl]-5,5-dimethyl-oxazolidin-2-one, p-toluenesulfonic acid salt of 

Downstream Products

• 1281973-31-6 C₂₀H₂₉N₃O₅ 
• 1101196-58-0 C₁₉H₂₇N₃O₅ 
• 1101196-52-4 C₂₀H₂₉N₃O₅ 
• 1101196-53-5 C₁₉H₂₆FN₃O₅ 
• 1101196-54-6 C₂₃H₃₃FN₄O₆ 
• 1101196-55-7 C₂₃H₃₃ClN₄O₆ 
• 1281973-26-9 C₂₅H₃₁N₃O₅ 
• 1101196-43-3 C₁₈H₂₅N₃O₅ 
• 1101196-81-9 C₂₆H₃₃N₃O₅ 
• 1101196-83-1 C₂₅H₃₀FN₃O₅ 
• 1281973-27-0 C₂₅H₂₉F₂N₃O₅ 
• 1101196-85-3 C₂₆H₃₃N₃O₆ 
• 1101196-87-5 C₂₉H₃₇FN₄O₆ 
• 1101196-88-6 C₂₉H₃₇ClN₄O₆ 

Relevant academic research and scientific papers

Peptide deformylase inhibitors

The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.

PEPTIDE DEFORMYLASE INHIBITORS

The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhi-bition of bacterial peptide deformylase (PDF) activity

Synthesis and in vitro antibacterial activity of oxazolidine LBM-415 analogs as peptide deformylase inhibitors

The drug resistant bacteria pose a severe threat to human health. The increasing resistance of those pathogens to traditional antibacterial therapy renders the identification of new antibacterial agents with novel antibacterial mechanisms an urgent need.

Peptide deformylase inhibitors of Mycobacterium tuberculosis: Synthesis, structural investigations, and biological results

Bacterial peptide deformylase (PDF) belongs to a subfamily of metalloproteases catalyzing the removal of the N-terminal formyl group from newly synthesized proteins. We report the synthesis and biological activity of highly potent inhibitors of Mycobacterium tuberculosis (Mtb) PDF enzyme as well as the first X-ray crystal structure of Mtb PDF. Structure-activity relationship and crystallographic data clarified the structural requirements for high enzyme potency and cell based potency. Activities against single and multi-drug-resistant Mtb strains are also reported.

A practical enantioselective synthesis of a novel peptide deformylase inhibitor

A practical synthesis of the peptide deformylase inhibitor LBM415,(2S)-N-(5-fluoro-1-oxido-2-pyridinyl)-1-[(2R)-2-[(formylhydroxyamino) methyl]-1-oxohexyl]-2-pyrrolidinecarboxamide, magnesium salt 11, is described. The key chiral intermediate, (2S)-N-(5-f

β-amino amides from β-lactams: Application to the formal synthesis of a peptide-deformylase inhibitor

A facile and a practical synthesis of peptide-deformylase inhibitor 1 is described using an acid-catalyzed aminolysis of β-lactam 12 with pyrrolidine 6 as the key transformation. In addition, simplified conditions for the conversion of a β-hydroxy acid to

PROCESS FOR PREPARING INTERMEDIATES USEFUL TO PREPARE CERTAIN ANTIBACTERIAL N-FORMYL HYDROXYLAMINES

The present invention is directed to a process for preparing intermediates that are useful to prepare certain antibacterial N-formyl hydroxylamine compounds which are peptide deformylase inhibitors.

Antibacterial agents

Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(═O) or the formula: —C(═O)NH(OH); R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(═O), a hydroxy, C1-C6 alkoxy, C1-C4 alkenyloxy, amino, C1-C4 alkylamino, or di-(C1-C6 alkyl)amino group; R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl(C1-C6 alkyl)- or aryl(C1-C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.

ANTIBACTERIAL AGENTS

Selected compounds of formula (I) are antibacterial agents: formula (I) wherein R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl (C1-C6 alkyl)- or aryl (C1-C6 /SUB

Asymmetric synthesis of BB-3497 - A potent peptide deformylase inhibitor

By screening a library of metalloenzyme inhibitors, the N-formyl-hydroxylamine derivative BB-3497 was identified as a potent inhibitor of Escherichia coli peptide deformylase with antibacterial activity both in vitro and in vivo. The homochiral synthesis of BB-3497, involving a novel asymmetric Michael addition reaction is described.