A novel series of aminotriazole-based P2X7 antagonists was synthesized, and their structure–activity relationships (SAR) were investigated for activity at both human and rat P2X7 receptors. Most compounds showed greater potency at the human receptor although several analogs were discovered with...

Two novel pseudopolymorphic copper complex crystals, [Cu(C14H8O2F3)2 (C2H6OS)2] (1) and [Cu(C14H8O2F3)2 (C3H7NO)] (2) were grown and characterized by UV–Vis, FTIR, EDS and single crystal XRD. With the aid of induced solvents, both complexes form different coordination sphere and exhibit the uni...

An efficient two-step approach for the synthesis of naphtho[1,2-b]furans and naphtho[2,1-b]furans has been developed. Various functionalized propargyl alcohols were etherified with α- or β-naphthol under Mitsunobu reaction conditions to give naphthyl 2-propynyl ethers, which underwent a facile...

Two new red-emitting Ir(III) complexes containing 2-(1-naphthyl)benzothiazole as cyclometalated ligands and the carrier transporting group-functionalized picolinate as ancillary ligands have been successfully synthesized and characterized. The Ir(III) complexes have good thermal stability with l...

A two-dimensional liquid chromatographic electrospray-ionization tandem mass spectrometric (LC/LC–ESI–MS/MS) procedure for the simultaneous determination of the expected mercapturic acids of naphthalene (1- and 2-naphthylmercapturic acids; 1- and 2-NpMA) and of the well-established parameter f...

A series of substituted styryl 2-hydroxy-1-naphthyl ketones have been synthesized by crossed-Aldol condensation reaction. These ketones are characterized by their physical constants, IR and NMR data. The IR carbonyl stretching and deformation modes ν (cm−1) of vinyl portion frequencies and 1H a...

A series of 2-naphthyl pyrazolines were synthesized by the cyclization of 2-naphthyl chalcones and phenylhydrazine hydrochloride in the presence of sodium acetate. The yields of pyrazoline derivatives are more than 80%. The synthesized pyrazolines were characterized by their physical constants, ...

New 1,2,4,5-tetrahydronaphtho[1,2-d]3,2-thiazepine 3,3-dioxides and 1,2,4,5-tetrahydronaphtho[2,1-d]3,4-thiazepine 3,3-dioxides were synthesized by aromatic intramolecular sulfonylamidomethylation of 2-(2-naphthyl) and 2-(1-naphthyl)ethanesulfonamides with s-trioxane using Amberlyst XN-1010 as c...

Microbial cultures produce complex and potentially interesting mixtures of biosynthetic intermediates and derivatives of metabolites. These mixtures’ reliable identification is important and so too is the development of techniques for their analysis. Here, a simple and highly selective method o...

Semi-pinacol cyclization of compound 8, having an acetal and an aldehyde substituent, was achieved by employing SmI2 and BF3·OEt2, leading to the highly stereoselective formation of cyclized product 9. The vicinal diol in 9 is discriminated, so as to allow selective glycosylation for the synthe...

By making use of the distance-dependent optical properties of gold nanoparticles as well as the mannose (Man)-specific binding ability of pradimicin (PRM), we have successfully developed a Man-recognizable chemosensor. The dissociation constant of the chemosensor for Man was estimated to be appr...

Actinomadura hibisca P157-2 produces potent antifungal antibiotic pradimicins. To enhance pradimicin production, ACCase from Streptomyces coelicolor and two regulatory genes metK1-sp and afsR-sp from Streptomyces peuticus were overexpressed into A. hibisca using an integration vector pSET152 und...

Pradimicins are potent antifungal antibiotics with effective inhibitory effects against HIV-1. Pradimicin A consists of an unusual dihydrobenzo[α]naphthacenequinone aglycone substituted with a combination of d-alanine and two sugar moieties. Detailed genetic studies revealed most steps in pradi...

Pradimicins A–C (1–3) are a group of antifungal and antiviral polyketides from Actinomadura hibisca. The sugar moieties in pradimicins are required for their biological activities. Consequently, the 5-OH that is used for glycosylation plays a critical role in pradimicin biosynthesis. A cytochr...

Pradimicins are antifungal and antiviral natural products from Actinomadura hibisca P157-2. The sugar moieties play a critical role in the biological activities of these compounds. There are two glycosyltransferase genes in the pradimicin biosynthetic gene cluster, pdmS and pdmQ, which are putat...

Pradimicins are a group of antiviral and antifungal natural products from Actinomadura hibisca. Two putative O-methyltransferase genes, pdmF and pdmT, are present in the pradimicin biosynthetic gene cluster. However, there is only one methoxy group (11-OCH3) in pradimicins. Through heterologous ...

SummaryNaturally occurring pradimicins (PRMs) show specific recognition of d-mannose (d-Man) in aqueous media, which has never been achieved by artificial small molecules. Although the Ca2+-mediated dimerization of PRMs is essential for their d-Man binding, the dimeric structure has yet to be el...

DNA-damaging agents are widely used in cancer therapy; however, their use is limited by dose-related toxicities, as well as the development of drug resistance. Drug discovery is essential to overcome these limitations and offer novel therapeutic options. In a previous study by our research group...

BackgroundIodine 123 (I-123) iomazenil is a specific ligand of the central benzodiazepine receptor, which is a part of the postsynaptic gamma-aminobutyric acid A receptor complex. We performed statistical image processing of I-123 iomazenil single-photon emission computed tomography to elucidate...

The effect of 1-amino-5-bromouracil (ABU), a novel central-acting agent, on monoaminergic neurotransmitter levels of rat brain was investigated. Under the nonstressed condition, ABU (20 and 30 mg/kg intraperitoneally [IP]) did not affect monoamine metabolism, whereas diazepam (5 mg/kg IP) increa...