The membrane modifying polyenes, filipin and nystatin, have been studied with respect to their ability to alter thyroid cell metabolism. Filipin, believed to modify membranes through interaction with phospholipids and/or cholesterol, appears to induce either no effect or mild inhibition of basel...

Adenyl cyclase activity was measured in washed ejaculated spermatozoa of the rhesus monkey (Macaca mulatta) by monitoring the conversion of [14C]ATP to [14C]cyclic 3′,5′-AMP. Thyroxine and triiodothyronine increase the accumulation of cyclic 3′,5′-AMP; other hormones, including androgens, go...

YM-09151-2, a novel benzamide derivative, significantly increased the concentrations of dopamine (DA) metabolites, both 3,4-dihydroxyphenylacetic acid and 3-methoxy-4-hydroxyphenylacetic acid (honovanillic acid). The maximum increase in such metabolites was about 4-fold the concentration in cont...

The sterile gene of YM-type thermo-sensitive male sterile wheat (Triticum aestivum L.) line has been mapped on chromosome arm 1BS, which was more than 10 cM distant from the adjacent molecular markers. For detecting markers with short distances to this gene, a population with 200 F2 plants was c...

The present study was designed to determine whether the 1-form of YM-12617, which was developed recently as an α1-adrenoceptor blocker, is capable of protecting the myocardium from hypoxia-induced disturbances of cardiac function and metabolism. Isolated rabbit hearts were perfused for 25 min u...

Efficient multimedia retrieval has become a vital issue because more audio and video data are now available. This paper focuses on content-based image retrieval (CBIR) in the compression domain (CPD). The retrieval features are extracted based on I-frame coding information in H.264. This paper p...

Various non-covalent interactions can be scrutinized by the measurement of physical properties. The nature of interactions between drugs and amino acids governs the functionalization process, so a better understanding demands reliable thermophysical data. Keeping this in mind, we report herein t...

The reaction between equimolar amounts of 3,4-epoxyperfluorooxolane and 3,3′,4,4′-tetraaminobiphenyl provided a new fluorine-containing diamino derivative of furoquinoxaline, namely, 6-(3,4-diaminophenyl)-1,1,3,3-tetrafluoro-1,3-dihydro-furo[3,4-b]quinoxaline. Its reactions with 3,4-epoxyperfl...

A new class of salen functionalized novel ligand N,N′-Bis(salicylidene)-9-(3,4-diaminophenyl)acridine, H2daasal (two potential intercalators, salen and acridine, which are linked together via C–C bond) and its metal complex [Ni(daasal)] have been synthesized and characterized by X-ray diffract...

A general method is described for the synthesis of 3-piperidine(methan)amines and their cyclic analogues. The 3,5-dichloro-2H-1,4-oxazin-2-ones 6 and 3-aryl substituted analogues are reacted with acetylenic dienophiles yielding pyridines. Further catalytic hydrogenation and functional group tran...

1,1,4,4-Tetrasubstituted cyclopenta[c]piperidines and the corresponding 4,4,7,7-pyrrolo[3,4-c]piperidines have been synthesised via cycloaddition of 5-chloro-6-methyl-3-phenyl-2H-1,4-oxazin-2-one with cyclopentene and 3-pyrroline derivatives, respectively, followed by reductive opening of the la...

The RET tyrosine kinase is an important therapeutic target for medullary thyroid cancer (MTC), and drug resistance mutations of RET, particularly V804M and V804L, are a main challenge for the current targeted therapy of MTC based on RET inhibitors. In this investigation, we report the structural...

3,5-Dichloro-2H-1,4-oxazin-2-ones 1 and 3-chloro-2H-1,4-benzoxazin-2-ones 2 react with α-aminoketones to yield bi- and tricyclic imidazo-fused intermediates via an intramolecular cyclisation reaction. Reaction of these lactone intermediates with various nucleophiles generates new substituted 1H...

By selective reaction of the chlorimine function in the adducts 2 from 3,5-dichloro-2H-1,4-oxazin-2-ones and double bond systems, a series of 6-substituted 2-oxa-5-azabicyclo[2.2.2]oct-5-en-3-ones 3 could be generated. Lactone cleavage of the latter with alcohols or amines yielded variously subs...

Selective functionalisation of the chlorimine group in 3,5-dichloro-6-methyl-2H-1,4-oxazin-2-one is usually realised in appropriate conditions, by electrophilic catalysis avoiding reaction of the lactone function. The azadiene system in the 3-substituted 5-chloro-6-methyl-2H-1,4-oxazin-2-ones is...

The SF5-analog of the Umemoto salt was synthesized in just two steps by combining our recently reported SF5-biaryl synthesis, via Suzuki coupling with 4-(pentafluorosulfanyl)benzenediazonium tetrafluoroborate, with Magnier's one-pot synthesis of dibenzothiophenium salts employing CF3SO2Na a...

The kinetic parameters were determined for C-trifluoromethylation of aniline with S-(trifluoromethyl)dibenzothiophenium triflate (1), its 3,7-dinitro derivative (2) and S-(trifluoromethyl)diphenylsulfonium triflate (3) in DMF-d7. The higher reactivity of heterocyclic 1 compared with non-heterocy...

New effective methods were developed for the preparation of useful electrophilic trifluoromethylating agents, S-(trifluoromethyl)dibenzothiophenium tetrafluoroborate (3) and triflate (4) and S-(trifluoromethyl)dibenzothiophenium-3-sulfonate (6). Thus, salts 3 and 4 were produced by the intramole...

1-Phenacyl-(1-azania-4-azabicyclo[2.2.2]octane) thiocyanate (PnDbSCN) and N-phenacyl-4-(N′,N′-dimethylamino)pyridinium thiocyanate (PnDpSCN) were prepared as novel photobase generators. These quaternary ammonium salts (QASs) have higher melting points and decomposition temperatures than corres...

We study thermal annealing-driven surface sealing of polymer hollow particles with a different surface property. Use of phase separation between polystyrene (PS) solid particles incorporated with sulfonate (SO3-) group and decane allows their transformation into hollow particles with an opening ...