80645

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Synthesis and in vitro antibacterial activity of quinolone/naphthyridone derivatives containing 3-alkoxyimino-4-(methyl)aminopiperidine scaffolds.

Kai Lv et al.

Bioorganic & medicinal chemistry letters, 23(6), 1754-1759 (2013-02-14)

We report herein the synthesis of a series of 7-[3-alkoxyimino-4-(methyl)aminopiperidin-1-yl]quinolone/naphthyridone derivatives. In vitro antibacterial activity of these derivatives was evaluated against representative strains, and compared with ciprofloxacin (CPFX), levofloxacin (LVFX) and gemifloxacin (GMFX). The results reveal that all of the

Microbial sensing by goblet cells controls immune surveillance of luminal antigens in the colon.

K A Knoop et al.

Mucosal immunology, 8(1), 198-210 (2014-07-10)

The delivery of luminal substances across the intestinal epithelium to the immune system is a critical event in immune surveillance, resulting in tolerance to dietary antigens and immunity to pathogens. How this process is regulated is largely unknown. Recently goblet

Sensitive and site-specific identification of carboxymethylated and carboxyethylated peptides in tryptic digests of proteins and human plasma.

Uta Greifenhagen et al.

Journal of proteome research, 14(2), 768-777 (2014-11-26)

Glycation refers to a nonenzymatic post-translational modification formed by the reaction of amino groups and reducing sugars. Consecutive oxidation and degradation can produce advanced glycation end products (AGEs), such as N(ε)-(carboxyethyl)lysine (CEL) and N(ε)-(carboxymethyl)lysine (CML). Although CEL and CML are

Development of potent antagonists for formyl peptide receptor 1 based on Boc-Phe-D-Leu-Phe-D-Leu-Phe-OH.

Ryo Hayashi et al.

Bioorganic & medicinal chemistry, 22(15), 3824-3828 (2014-07-19)

While stimulation of formyl peptide receptors (FPRs) on the surface of human neutrophils induces several immune responses, under conditions of continuous activation of the receptor by agonists such as formyl-Met-Leu-Phe-OH (fMLP), neutrophil-dependent tissue damage ensues. Thus, FPR antagonists could be

[Piperidine in the brain: its neurobiological significance].

Y Kasé et al.

Yakubutsu, seishin, kodo = Japanese journal of psychopharmacology, 9(3), 257-271 (1989-09-01)

Piperidine (Pip) is a normal constituent in mammalian brain, affects synaptic mechanism in the CNS, and influences neural mechanisms governing regulation of emotional behavior and extrapyramidal function. In addition, there are enzyme systems within the brain that synthesize and metabolize

Total synthesis of (-)-kopsinine by an asymmetric one-pot [n+2+3] cyclization.

Shingo Harada et al.

Chemistry, an Asian journal, 7(10), 2196-2198 (2012-08-22)

Antimicrobial properties of membrane-active dodecapeptides derived from MSI-78.

Claudia Monteiro et al.

Biochimica et biophysica acta, 1848(5), 1139-1146 (2015-02-15)

Antimicrobial peptides (AMPs) are a class of broad-spectrum antibiotics known by their ability to disrupt bacterial membranes and their low tendency to induce bacterial resistance, arising as excellent candidates to fight bacterial infections. In this study we aimed at designing

Molybdenum trioxide nanoparticles with intrinsic sulfite oxidase activity.

Ruben Ragg et al.

ACS nano, 8(5), 5182-5189 (2014-04-08)

Sulfite oxidase is a mitochondria-located molybdenum-containing enzyme catalyzing the oxidation of sulfite to sulfate in the amino acid and lipid metabolism. Therefore, it plays a major role in detoxification processes, where defects in the enzyme cause a severe infant disease

Design, synthesis and biological evaluation of novel pyrenyl derivatives as anticancer agents.

Debasish Bandyopadhyay et al.

European journal of medicinal chemistry, 89, 851-862 (2014-12-03)

Polycyclic aromatic hydrocarbons are widespread in nature with a toxicity range from non-toxic to extremely toxic. A series of pyrenyl derivatives has been synthesized following a four-step strategy where the pyrene nucleus is attached with a basic heterocyclic moiety through

Qualitative and quantitative determination of peptides related to celiac disease in mixtures derived from different methods of simulated gastrointestinal digestion of wheat products.

Barbara Prandi et al.

Analytical and bioanalytical chemistry, 406(19), 4765-4775 (2014-05-21)

During wheat digestion, gluten-derived proteolytic resistant peptides are generated, some of them involved in celiac disease. In vitro digestion models able to mimic the peptides generated in the human gastrointestinal tract are extremely useful to assess the pathogenicity of wheat-derived

Probe-inspired nano-prodrug with dual-color fluorogenic property reveals spatiotemporal drug release in living cells.

Xiangdong Xue et al.

ACS nano, 9(3), 2729-2739 (2015-02-18)

The versatility of the fluorescent probes inspires us to design fluorescently traceable prodrugs, which enables tracking the drug delivery kinetics in living cells. Herein, we constructed a self-indicating nanoprodrug with two fluorescent moieties, an aggregation-induced emission molecule (tetraphenylethylene, TPE) and

Comparison of capillary electrophoresis-mass spectrometry and hydrophilic interaction chromatography-mass spectrometry for anionic metabolic profiling of urine.

Miranda G M Kok et al.

Talanta, 132, 1-7 (2014-12-06)

In order to assess the utility of a recently developed capillary electrophoresis-mass spectrometry (CE-MS) method for the study of anionic metabolites in urine, a comparison was made with hydrophilic interaction chromatography-MS (HILIC-MS) using negative electrospray ionization. After optimization of the

Heparin octasaccharide decoy liposomes inhibit replication of multiple viruses.

Gabriel L Hendricks et al.

Antiviral research, 116, 34-44 (2015-02-01)

Heparan sulfate (HS) is a ubiquitous glycosaminoglycan that serves as a cellular attachment site for a number of significant human pathogens, including respiratory syncytial virus (RSV), human parainfluenza virus 3 (hPIV3), and herpes simplex virus (HSV). Decoy receptors can target

Receptor-mediated uptake of boron-rich neuropeptide y analogues for boron neutron capture therapy.

Verena M Ahrens et al.

ChemMedChem, 10(1), 164-172 (2014-10-24)

Peptidic ligands selectively targeting distinct G protein-coupled receptors that are highly expressed in tumor tissue represent a promising approach in drug delivery. Receptor-preferring analogues of neuropeptide Y (NPY) bind and activate the human Y1 receptor subtype (hY1 receptor), which is

Three-dimensional quantitative structure-activity relationship analyses of substrates of the human proton-coupled amino acid transporter 1 (hPAT1).

Iris Thondorf et al.

Bioorganic & medicinal chemistry, 19(21), 6409-6418 (2011-10-01)

The proton-coupled amino acid transporter hPAT1 has recently gained much interest due to its ability to transport small drugs thereby allowing their oral administration. A three-dimensional quantitative structure-activity relationship (3D QSAR) study has been performed on its natural and synthetic

Sequence and length optimization of membrane active coiled coils for triggered liposome release.

Camilla Skyttner et al.

Biochimica et biophysica acta. Biomembranes, 1861(2), 449-456 (2018-11-14)

Defined and tunable peptide-lipid membrane interactions that trigger the release of liposome encapsulated drugs may offer a route to improving the efficiency and specificity of liposome-based drug delivery systems, but this require means to tailor the performance of the membrane

Inhibition of COX-2-mediated eicosanoid production plays a major role in the anti-inflammatory effects of the endocannabinoid N-docosahexaenoylethanolamine (DHEA) in macrophages.

Jocelijn Meijerink et al.

British journal of pharmacology, 172(1), 24-37 (2014-05-02)

N-docosahexaenoylethanolamine (DHEA) is the ethanolamine conjugate of the long-chain polyunsaturated n-3 fatty acid docosahexaenoic (DHA; 22: 6n-3). Its concentration in animal tissues and human plasma increases when diets rich in fish or krill oil are consumed. DHEA displays anti-inflammatory properties

Piperazine and piperidine triazole ureas as ultrapotent and highly selective inhibitors of monoacylglycerol lipase.

Niina Aaltonen et al.

Chemistry & biology, 20(3), 379-390 (2013-03-26)

Monoacylglycerol lipase (MAGL) terminates the signaling function of the endocannabinoid, 2-arachidonoylglycerol (2-AG). During 2-AG hydrolysis, MAGL liberates arachidonic acid, feeding the principal substrate for the neuroinflammatory prostaglandins. In cancer cells, MAGL redirects lipid stores toward protumorigenic signaling lipids. Thus MAGL

Discovery and lead optimization of a novel series of CC chemokine receptor 1 (CCR1)-selective piperidine antagonists via parallel synthesis.

Cullen L Cavallaro et al.

Journal of medicinal chemistry, 55(22), 9643-9653 (2012-10-19)

A series of novel, potent CCR1 inhibitors was developed from a moderately active hit using an iterative parallel synthesis approach. The initial hit (composed of three subunits: an amine, a central amino acid, and an N-terminal cap) became the basis

Dipeptidyl peptidase IV as a potential target for selective prodrug activation and chemotherapeutic action in cancers.

Arik Dahan et al.

Molecular pharmaceutics, 11(12), 4385-4394 (2014-11-05)

The efficacy of chemotherapeutic drugs is often offset by severe side effects attributable to poor selectivity and toxicity to normal cells. Recently, the enzyme dipeptidyl peptidase IV (DPPIV) was considered as a potential target for the delivery of chemotherapeutic drugs.

Preparation and spectral characterization of fluorescence probes based on 4-N,N-dimethylamino benzoic acid and sterically hindered amines.

Csaba Kósa et al.

Journal of fluorescence, 22(5), 1371-1381 (2012-06-26)

The adducts of simple chromophore 4-N,N-dimethylamino benzoic acid with 2,2,6,6-tetrametyl-4-hydroxy- or 4-amino-piperidine were examined as fluorescence probes (spin double sensors) to monitor radical processes. The links in the adducts were either an ester or amide group, and the sterically hindered

Intracellular delivery of therapeutic antisense oligonucleotides targeting mRNA coding mitochondrial proteins by cell-penetrating peptides.

Carmine Pasquale Cerrato et al.

Journal of materials chemistry. B, 8(47), 10825-10836 (2020-11-12)

Cell-penetrating peptides are a promising therapeutic strategy for a wide variety of degenerative diseases, ageing, and cancer. Among the multitude of cell-penetrating peptides, PepFect14 has been preferentially used in our laboratory for oligonucleotide delivery into cells and in vivo mouse

Quantification of plasma HIV RNA using chemically engineered peptide nucleic acids.

Chao Zhao et al.

Nature communications, 5, 5079-5079 (2014-10-07)

The remarkable stability of peptide nucleic acids (PNAs) towards enzymatic degradation makes this class of molecules ideal to develop as part of a diagnostic device. Here we report the development of chemically engineered PNAs for the quantitative detection of HIV

The discovery of CCR3/H1 dual antagonists with reduced hERG risk.

Ash Bahl et al.

Bioorganic & medicinal chemistry letters, 22(21), 6688-6693 (2012-10-04)

A series of dual CCR3/H(1) antagonists based on a bispiperidine scaffold were discovered. Introduction of an acidic group overcame hERG liability. Bioavailability was optimised by modulation of physico-chemical properties and physical form to deliver a compound suitable for clinical evaluation.

Rationally designed peptoids modulate aggregation of amyloid-beta 40.

J Phillip Turner et al.

ACS chemical neuroscience, 5(7), 552-558 (2014-04-03)

Alzheimer's disease (AD) is the most common form of dementia and the sixth leading cause of death in the United States. Plaques composed of aggregated amyloid-beta protein (Aβ) accumulate between the neural cells in the brain and are associated with

The many roles for fluorine in medicinal chemistry.

William K Hagmann

Journal of medicinal chemistry, 51(15), 4359-4369 (2008-06-24)

Synthesis and structure-activity relationship of piperidine-derived non-urea soluble epoxide hydrolase inhibitors.

Stevan Pecic et al.

Bioorganic & medicinal chemistry letters, 23(2), 417-421 (2012-12-15)

A series of potent amide non-urea inhibitors of soluble epoxide hydrolase (sEH) is disclosed. The inhibition of soluble epoxide hydrolase leads to elevated levels of epoxyeicosatrienoic acids (EETs), and thus inhibitors of sEH represent one of a novel approach to

Chemical probes of a trisubstituted pyrrole to identify its protein target(s) in Plasmodium sporozoites.

Tyrell Towle et al.

Bioorganic & medicinal chemistry letters, 23(6), 1874-1877 (2013-02-12)

Malaria is a disease that has a major impact in many developing nations, especially on the African continent. There is a need to develop new therapeutics and prophylactic treatments against it. A trisubstituted pyrrole was recently found to inhibit infection

Synthetic analogs of anoplin show improved antimicrobial activities.

Jens K Munk et al.

Journal of peptide science : an official publication of the European Peptide Society, 19(11), 669-675 (2013-09-11)

We present the antimicrobial and hemolytic activities of the decapeptide anoplin and 19 analogs thereof tested against methicillin-resistant Staphylococcus aureus ATCC 33591 (MRSA), Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853), vancomycin-resistant Enterococcus faecium (ATCC 700221) (VRE), and Candida albicans

Pyrrolidine, piperidine, and pyridine alkaloids.

A R Pinder

Natural product reports, 6(5), 515-521 (1989-10-01)

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