83436-46-8Relevant academic research and scientific papers
N- and C-terminal modifications of negamycin
Raju,Mortell, Kathleen,Anandan, Sampathkumar,O'Dowd, Hardwin,Gao, Hongwu,Gomez, Marcela,Hackbarth, Corinne,Wu, Charlotte,Wang, Wen,Yuan, Zhengyu,White, Richard,Trias, Joaquim,Patel, Dinesh V.
, p. 2413 - 2418 (2007/10/03)
Negamycin 1 is a bactericidal antibiotic with activity against Gram-negative bacteria, and served as a template in an antibiotic discovery program. An orthogonally protected β-amino acid derivative 3a was synthesized and used in parallel synthesis of negamycin derivatives on solid support. This advanced intermediate was also used for N- and C-terminal modifications using solution-phase methodologies. The N-terminal modifications have resulted in the identification of active analogues, whereas the C-terminal modifications resulted in complete loss of antibacterial activity. The N-methyl negamycin analogue, 19a, inhibits protein synthesis (IC50=2.3 μM), has antibacterial activity (Escherichia coli, MIC=16 μg/mL), and is efficacious in an E. coli murine septicemia model (ED50=16.3 mg/kg).
Peptidyl β-homo-aspartals: Specific inhibitors of interleukin-1β converting enzyme and its homologues (caspases)
Bajusz, Sandor,Fauszt, Iren,Nemeth, Klara,Barabas, Eva,Juhasz, Attila,Patthy, Miklos
, p. 1477 - 1482 (2007/10/03)
Inhibition of interleukin-1β convening enzyme (ICE), apopain, papain, thrombin and trypsin with substrate like peptidyl L- and D-α-aldehydes and their L-β-homo-aldehyde analogues was investigated. The L-β-homo-aspartals appear to be specific inhibitors fo
