Peptide deformylase inhibitor

DESIGN AND SAR OF PEPTIDE DEFORMYLASE INHIBITORS Early Substrate-based Inhibitors... 

Peptide deformylase inhibitors, 44 (2006) 109 Peroxisome proliferator-acrtvated receptor gamma (PPARy) ligands, 42 (2004) 1 Pharmacology of Alzheimer s disease,... 

Peptide Deformylase Inhibitors as Novel Antibacterial Agents. 183... 

In an effort to access peptide-deformylase inhibitor 85, Prasad [96] has described the aminolysis of /V-benzyloxy (3-lactam 86 with proline derivative 87 to give the (3-(0-benzyl hydroxylamine) amide 88. It is worth noting that no acyl activation of the (3-lactam nitrogen is operating in this case. After examination of an array of solvents and additives for the ring opening, the best result (>96% yield) was finally obtained with 2-ethylhexanoic acid as the catalyst, and THF was the preferred solvent at 72°C (Scheme 29). 

Clements, J.M. et al. 2001. Antibiotic activity and characterization of BB-3497, a novel peptide deformylase inhibitor. Antimicrob. Agents Chemother. 45, 563-570. 

Hackbarth, C.J. et al. 2002. V-alkyl urea hydroxamic acids as a new class of peptide deformylase inhibitors with antibacterial activity. Antimicrob. Agents Chemother. 46, 2752-2764. 

Rosse et al. described the oxidation of the resin-bound /3-sulfenyl hydroxamic acids A -sulfonyloxaziridines <2001SL538>. For example, oxidation of 143 with 33 afforded the corresponding sulfoxide 144 in 71% yield after cleavage of the resin with TFA. Apfel et al. in the preparation of some potent peptide deformylase inhibitors and antibacterial agents employed a similar transformation<2000JME2324>. 

Clements, J. M., Ayscough, A. P., Keavey, K., and East, S. P. (2002) Peptide deformylase inhibitors, potential for a new class of broad spectrum antibacterials. Curr. Med. Chem. Antiinfect. Agents 1, 239-249. 

Clements JM, Beckett RP, Brown A, Gr C, LobeU M, Palan S, Thomas W, Whittaker M, Wood S, SalamaS, Baker PJ, Rodgers HP, Barynin V, Rice DW, Hunter MG (2001) Antibiotic activity and characterization of BB-3497, a novel peptide deformylase inhibitor. Antimicrob Agents Chemother 45 563-570... 

D.R.P. Guay, Drug forecase - the peptide deformylase inhibitors as antibacterial agents, Ther. Clin. RiskManag. 3 (4) (2007) 513-525. 

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