- CARBAPENEM ANTIBACTERIALS WITH GRAM-NEGATIVE ACTIVITY
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The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.
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- Nitrilase-catalyzed enantioselective synthesis of pyrrolidine- And piperidinecarboxylic acids
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The enantioselective synthesis of the nonproteinogenic amino acids β-proline and nipecotic acids from their readily available nitriles is achieved in high enantiomeric excess by commercially available nitrilases. The presented procedure comprises not more than 4 steps, thus considerably reducing the multiple steps generally required. Amide formation is also observed for specific heterocyclic nitriles.
- Winkler, Margit,Meischler, Dorith,Klempier, Norbert
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p. 1475 - 1480
(2008/09/16)
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- PYRROLIDINE DERIVATIVES AS HISTAMINE RECEPTORS LIGANDS
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The present invention relates to pyrrolidine derivatives of formula (I) having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.
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Page/Page column 22-23
(2010/11/08)
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- Stability against enzymatic hydrolysis of endomorphin-1 analogues containing β-proline
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The enantiomer of endomorphin-1 (Tyr-Pro-Trp-PheNH2) and the analogues containing (S)-or (R)-β-proline have been synthesized, and their affinities towards μ-opioid receptors have been measured. As expected, the incubations of the different peptides with some commercially available enzymes showed that the presence of D-residues gave strong resistance towards digestion. The presence of β-proline alone is sufficient to confer good resistance against the hydrolysis of the biologically strategic Pro-Trp bond.
- Cardillo, Giuliana,Gentilucci, Luca,Tolomelli, Alessandra,Calienni, Maria,Qasem, Ahmed R.,Spampinato, Santi
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p. 1498 - 1502
(2007/10/03)
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- Synthesis of potent oxindole CDK2 inhibitors
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A series of oxindole CDK2 inhibitors was synthesized. These novel analogues have a saturated monosubstituted cyclic moiety at their C-4 position that mimics the ribofuranoside of ATP. This substitution afforded agents with increased potency relative to th
- Dermatakis, Apos,Luk, Kin-Chun,DePinto, Wanda
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p. 1873 - 1881
(2007/10/03)
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- Synthesis and binding activity of endomorphin-1 analogues β-amino acids
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Endomorphin-1 (Tyr-Pro-Trp-PheNH2) has been proposed as the most potent endogenous ligand of the μ-opioid receptors. In this paper, we describe the synthesis of some endomorphin-1 based tetrapeptides in which a residue of the sequence Tyr-Pro-Trp-PheNH2 is replaced by the corresponding β-isomer. These novel peptides showed different affinities for the opioid receptors labeled with [3H]-DAMGO in rat brain membranes, depending on the β-amino acid. In particular, the tetrapeptide containing β-Pro (Tyr-β-(R)-Pro-Trp-PheNH2) displayed a higher affinity than endogenous endomorphin-1, as revealed by their K(i) values (0.33 and 11.1 nM, respectively). (C) 2000 Elsevier Science Ltd.
- Cardillo, Giuliana,Gentilucci, Luca,Melchiorre, Paolo,Spampinato, Santi
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p. 2755 - 2758
(2007/10/03)
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- Constrained β-alanine based GpIIb/IIIa antagonists
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The concepts of centrally constrained and peptide based fibrinogen receptor antagonists have been successfully combined into a single series of analogs which have been demonstrated to be potent inhibitors of platelet aggregation.
- Klein, Scott I.,Czekaj, Mark,Molino, Bruce F.,Valeria, Chu
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p. 1773 - 1778
(2007/10/03)
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