The six N-(dimethoxybenzyl)-4-bromo-2,5-dimethoxyphenethylamine regioisomers are potential designer compounds related to the common NBOMe drug N-(2-methoxy)benzyl-4-bromo-2,5-dimethoxyphenethylamine (25B-NBOMe). These six compounds represent the incorporation of one additional methoxy-group into...
The reactions of 1,1-diacetylcyclopropane (1) with a number of hydrazine and hydroxylamine derivatives proceed via cyclopropane ring opening with incorporation of external nucleophile (solvent) to give the 4-β-X-ethyl derivatives of 3,5-dimethylpyrazoles and -isoxazoles, a novel route to these ...
A variety of fused 3-amino-1,2,4-triazole derivatives were synthesized via addition of aryl hydrazines to isothiocyanates followed by I2-mediated oxidative cyclodesulfurization. This transition-metal-free synthetic process provides facile access to 1,2,4-triazolo[4,3-a]pyridines and related hete...
The mode of inactivation of herpes simplex virus type 1 and human ribonucleotide reductases by 2-acetylpyridine 5-[(2-chloroanillino)-thiocarbonyl]-thiocarbonohydrazone (348U87) was determined and compared to that described previously [Porter et al. Biochem Pharmacol39: 639–646, 1990] for 2-ace...
Clarithromycin is a semi-synthetic antibiotic. High-performance liquid chromatography is used to identify and estimate both manufacturing and degradation impurities. The sample is chromatographed on a YMCC18 column using an eluent of acetonitrile—0.033 M KH2PO4 (48:52) at an apparent pH of 5.4 ...
Chlorobenzene (CB) was administered to male Wistar rats. Twenty-four-hour urine samples were collected over a period of 7 days. p-Chlorophenylmercapturic acid, chlorophenols and a guanine adduct were determined by chromatographic methods. The excretion pattern of p-chlorophenylmercapturic acid d...
When N-acetyl-S-(2-hydroxy-4-bromocyclohexa-3,5-dienyl)-l-cysteine (4-S-premercapturic acid) and ifN-acetyl-S-hydroxy-5-bromocyclohexa-3,5-dienyl)-l-cysteine (3-S-premercapturic acid) were used as substrates in incubations with Hartley guinea pig kidney 9000 g supernatant preparations, the major...
In this work, the α-cluster formation problem for nuclei in the “island” of light α-emitters ranging from tellurium to barium is revisited by using the latest experimental decay data in AME2016. We show in a qualitative way that the α-cluster preformation probability (Pα) is significantly ...
N-chloro-amino acids are readily formed in chlorination water treatment technologies. These reactions are also important in biological systems where HOCl plays an important role in the defense mechanism against invading pathogens. The intermediates and the products formed are of primary concern ...
N-Alkylated-α-amino acids are useful building blocks for the pharmaceutical and fine chemical industries. Enantioselective methods of N-alkylated-α-amino acid synthesis are therefore highly valuable and widely investigated. While there are a variety of chemical methods for their synthesis, the...
Antiproliferative activity of twenty-nine (E)-4-aryl-4-oxo-2-butenoic acid amides against three human tumor cell lines (HeLa, FemX, and K562) is reported. Compounds showed antiproliferative activity in one-digit micromolar to submicromolar concentrations. The most active derivatives toward all t...
Pasteurella multocida is among the most important respiratory pathogens of cattle. Outer-membrane protein (OmpH) constitutes an essential bacterial antigen and is well studied in avian bacterial strains. Studies on isolates from cattle with signs of respiratory disease caused by Pasteurella mult...
Today, there is an increasing emphasis on recombinant vaccines to eliminate the side effects of conventional vaccines such as whole-cell bacteria. Query fever is an emerging disease that causes irreparable complications for both humans and domestic animals. The cause of this disease is Coxiella ...
Infectious bursal disease virus (IBDV) is a highly contagious disease that results in enormous economic losses in the global poultry sector. Lactic acid bacteria are an appealing vehicle for the safe and effective delivery of heterologous protein antigens. Oral administration of the commensal ba...
Iron bioavailability is crucial for mitochondrial metabolism and biosynthesis. Dysregulation of cellular iron homeostasis affects multiple aspects of mitochondrial physiology and cellular processes. However, the intracellular iron trafficking pathway in Candida albicans remains unclear. In this ...
Gram-positive bacteria deploy the type VII secretion system (T7SS) to facilitate interactions between eukaryotic and prokaryotic cells. In recent work, we identified the TelC protein from Streptococcus intermedius as a T7SS-exported lipid II phosphatase that mediates interbacterial competition. ...
The APSES protein family belongs to transcriptional factors of the basic helix-loop-helix (bHLH) class, the originally described members (APSES: Asm1p, Phd1p, Sok2p, Efg1p and StuAp) are used to designate this group of proteins, and they have been identified as key regulators of fungal developme...
The genome of aureophage Phi11 reveals the presence of the gene gp07 which codes for the putative antirepressor protein (GenBank accession no. NC_004615.1). Antirepressor proteins are mainly involved in lytic cycle determination mechanisms of various bacteriophages. The Phi11 protein Gp07 consis...
WNT-3A is a secreted lipoglycoprotein that engages Class Frizzled receptors and LDL receptor related protein 5/6 (LRP5/6) for cellular communication. Generally, WNT-3A mediates WNT/β-catenin signaling to regulate TCF/LEF-dependent gene expression. We have previously shown that β-catenin levels...
Wnt-3a and Wnt-5a signaling activities inhibit and promote neurite outgrowth, respectively, to regulate dendritic and axonal genesis during neurodevelopment. NF-α1, a neurotrophic factor, has been shown to modulate dendritic remodeling and negatively regulate the canonical Wnt-3a pathway. Here,...
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