1,720,974 research outputs found
Synthesis of Short Cationic Antimicrobial Peptidomimetics Containing Arginine Analogs
No full textWorldwide efforts are underway to develop new antimicrobial agents against bacterial resistance. To identify new compounds with
a good antimicrobial profile, we designed and synthesized two series of small cationic antimicrobial peptidomimetics (1–8)
containing unusual arginine mimetics (to introduce cationic charges) and several aromatic amino acids (bulky moieties to
improve lipophilicity). Both series were screened for in vitro antibacterial activity against a representative panel of Gram-positive
(Staphylococcus aureus and Staphylococcus epidermidis) and Gram-negative (Escherichia coli and Klebsiella pneumoniae) bacterial
strains, and Candida albicans. The biological screening showed that peptidomimetics containing tryptophan residues are
endowed with the best antimicrobial activity against S. aureus and S. epidermidis in respect to the other synthesized derivatives
(MIC values range 7.5–50mg/ml). Moreover, small antimicrobial peptidomimetics derivatives 2 and 5 showed an appreciable
activity against the tested Gram-negative bacteria and C. albicans. The most active compounds (1–2 and 5–6) have been tested
against Gram-positive established biofilm, too. Results showed that the biofilm inhibitory concentration values of these
compounds were never up to 200mg/ml. The replacement of tryptophan with phenylalanine or tyrosine resulted in considerable
loss of the antibacterial action (compounds 3–4 and 7–8) against both Gram-positive and Gram-negative bacterial strains.
Furthermore, by evaluating hemolytic activity, the synthesized compounds did not reveal cytotoxic activities, except for
compound 5. Copyright © 2012 European Peptide Society and John Wiley & Sons, Ltd.
Keywords: antimicrobial peptidomimetics; arginine analogs; antibacterial activity; antifungal activity; microbia
N-(tert)-Butyloxycarbonyl-beta,beta-Cyclopentyl-Cysteine (Acetamidomethyl)-Methyl Ester for Synthesis of Novel Peptidomimetic Derivatives
No full textN-Acetyl-L-Methionyl-L-Dopa-Methyl Ester as a dual acting drug that relieves L-Dopa-induced oxidative toxicity
No full textInitiation and progression of Parkinson's disease seem to be linked to oxidative stress, closely related to
decreased mitochondrial functions and ubiquitin proteasome system dysfunction. To date, L-Dopa is the most
effective medication , although long-term treatment can enhance oxidative stress and accelerate the
degenerative process of residual cells. Therefore the inhibition of oxidation of L-Dopa/dopamine and the
inhibition of reactive oxygen species formation are important strategies for neuroprotective therapy. Recently,
several dual acting drugs, in which L-Dopa/dopamine are covalently linked to antioxidant molecules, were
shown to induce sustained delivery of both L-Dopa/dopamine in rat plasma and striatum, suggesting that
these compounds might be proposed as useful agents against Parkinson's disease. Here, by analyzing GSH
levels and heme oxygenase-1 expression, we investigated in primary mesencephalic neuron cultures and in
newborn mice the effects of the treatment with Ac-Met-LD-OMe. Moreover, by using proteasome inhibitortreated
mice as Parkinson's disease animal model, we demonstrated the beneficial effects of the systemic
administration of this novel codrug
A Potent (R)-alpha-bis-lipoyl Derivative Containing 8-Hydroxyquinoline Scaffold: Synthesis and Biological Evaluation of Its Neuroprotective Capabilities in SH-SY5Y Human Neuroblastoma Cells
No full textA novel bis-lipoyl derivative containing 8-hydroxyquinoline scaffold (LA-HQ-LA, 5) was synthesized as a new multifunctional drug candidate with antioxidant, chelant, and neuroprotective properties for the treatment of neurodegenerative diseases. We have investigated the potential effectiveness of LA-HQ-LA against the cytotoxicity induced by 6-OHDA and H2O2 on human neuroblastoma SH-SY5Y cell line. Our outcomes showed that LA-HQ-LA resulted in significant neuroprotective and antioxidant effects against H2O2- and 6-OHDA-induced neurotoxicity in human neuroblastoma SH-SY5Y cells, as assessed by MTT assay. In particular, it showed potent neuroprotective effects against 6-OHDA in RA/PMA differentiated cells at all the tested concentrations.
(This article belongs to the Special Issue CNS-Drugs and Therapy
N-(tert-butilossicarbonil)-beta,beta-ciclopentil-cisteina (acetamidometil)-metil estere per la sintesi di nuovi derivati peptidomimetici
No full textNew pharmacologic tools against Parkinson's disease: L-Dopa-antioxidant codrugs containing the methionine residue
No full text
Going Beyond Counting First Authors in Author Co-citation Analysis
Full text linkThe present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation
counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings
are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that
only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into
account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
- …
