Showing 1-30 of 74 results for "80645"
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.
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...
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...
Pyrrolidine, piperidine, and pyridine alkaloids.
A R Pinder
Natural product reports, 6(5), 515-521 (1989-10-01)
The many roles for fluorine in medicinal chemistry.
William K Hagmann
Journal of medicinal chemistry, 51(15), 4359-4369 (2008-06-24)
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...
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...
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...
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...
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...
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...
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....
Li Wang et al.
Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy, 105, 62-66 (2013-01-09)
A piperidine-modified calix[4]arene derivative was synthesized and its structure was confirmed with X-ray diffraction data. UV-visible spectroscopy was used to study its molecular recognition of rare earth ions. The results revealed the calix[4]arene derivative could separate tight metal picrate ion...
Sachiro Kakinoki et al.
Acta biomaterialia, 13, 42-51 (2014-12-03)
Mechanotransduction in the regulation of cellular responses has been previously studied using elastic hydrogels. Because cells interact only with the surface of biomaterials, we are focusing on the molecular mobility at the outermost surface of biomaterials. In this study, surfaces...
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...
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...
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...
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...
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...
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...
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)
Nafizal Hossain et al.
Bioorganic & medicinal chemistry letters, 23(6), 1883-1886 (2013-02-19)
Conformationally constrained spirocycles (17-23) and (31-36) were synthesised. In vitro data revealed that these compounds are CCR1 antagonists with sub-nanomolar potency. In a functional assay 22, 23 and 36 inhibited CCR1 mediated chemotaxis with an IC50 value of 2, 2.6...
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...
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...
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...
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...
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...
Almeqdad Y Habashneh et al.
Archiv der Pharmazie, 347(6), 415-422 (2014-03-13)
A new series of N1-(flavon-6-yl)amidrazones were synthesized by reacting the hydrazonoyl chloride derived from 6-aminoflavone with the appropriate sec-cyclic amines. The antitumor activities of these compounds were evaluated on breast cancer (MCF-7) and leukemic (K562) cell lines. Among the compounds...
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...
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...

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