Chiral C2-symmetric diphenylthiophosphoramide ligand L1 prepared from C2-symmetric (1S,2S)-(−)-1,2-diphenylethylenediamine was found to be a fairly effective chiral ligand for Cu(I)-promoted 1,3-dipolar cycloaddition of imines and pyrrole-2,5-dione derivatives to give the corresponding adducts i...

A new accepter unit, pyrrolo[3,2-b]pyrrole-2,5-dione, deserves much attention as the electron-deficient unit for the generation of electron donor material for organic photovoltaic cells (OPVs). Pyrrolo[3,2-b]pyrrole-2,5-dione unit, regioisomer of the known pyrrolo[3,4-c]pyrrole-1,4-dione, is ori...

Excess lipid accumulation in the arterial intima and formation of macrophage-derived foam cells in the plaque could cause atherosclerotic lesion. Cholesterol absorption inhibitors could suppress the lipid accumulation of human macrophage, inflammatory response and the development of atherosclero...

The direct preparation of chiral 2,2′-bipyridine bis-N-oxides has been developed. The method involves two stages, first, the deprotonation of substituted chiral pyridine N-oxides and second, the oxidative dimerization of the resulting 2-lithiopyridine N-oxides. Optimization of the reaction cond...

The chemistry of the iron complexes of two Schiff-base ligands namely, N-2-mercaptophenyl-2′-pyridylmethylenimine (PyASH, 1) and N-2-mercapto-2-methylpropyl-2′-pyridylmethylenimine (PyMSH, 2) has been explored in a systematic manner. Use of DMF as solvent allows one to isolate the Fe(II) compl...

A Cu(I)-catalyzed asymmetric aziridination of styrenes with a chiral N-tosyloxycarbamate has been developed. Double stereodifferentiation was observed and both the N-tosyloxycarbamate substituent and the bis(oxazoline) ligand have a significant effect on the yields and diastereoselectivities. Th...

The acid-base properties of N,N′-disubstituted dithiooxamides derived from alkyl-α-aminoacids or glycylglycine were studied in aqueous solutions of pH 2.5-10.8. For each dithiooxamide, protonation constants were obtained from potentiometric data for three dilute aqueous solutions [I=0.15 M (Na...

Treatment of metalloligand [Ni(tsalphen)] (tsalphen = N,N′-bis(2-thiobenzylidene)-1,2-phenylenediaminato) with [(η6-p-cymene)RuCl(μ-Cl)]2 or [CpRu(PPh3)2Cl] afforded cationic “Ni(μ-S)2Ru” bimetallic complexes [(η6-p-cymene)Ru{Ni(tsalphen)}(MeCN)](OTf)2 (1) and [CpRu{Ni(tsalphen)}(PPh3)]2(...

The asymmetric direct bisvinylogous conjugate addition of 5-benzylfurfural derivatives to nitroalkenes using a thiourea organocatalyst resulted in a corresponding ε-regioselective addition products in high yields and up to 95% enantiomeric excess.

Caffeic acid phenethyl ester (CAPE) is a bioactive polyphenolic compound obtained from propolis extract. Although it has a broad therapeutic potential, the bioavailability of CAPE is limited, due to reduced solubility and poor plasmatic stability. Efforts to reduce these pharmacokinetic drawback...

Various new chiral thioureas have been synthesized and used as ligands for the asymmetric hydroformylation of styrene catalyzed by rhodium(I) complexes. The best results were obtained with N-phenyl-N′-(S)-(1-phenylethyl)-thiourea associated to a cationic rhodium(I) precursor, and asymmetric ind...

Computer-aided drug design has advanced by leaps and bounds, and has been widely used in various fields, and especially in the field of drug discovery. Although the crystal structure of the gibberellin (GA) receptor GID1A had been reported in previous studies, there is still a lack of designs of...

Several single enantiomer thioureas have been synthesized and have been converted to their cyclic derivatives: 2-imino-thiazolidin-4-ones. The conformations of the thioureas have been determined in solution and in the solid state. In solution; an interconversion between the E,Z and Z,E conformat...

A series of α-substituted N-(4-tert-butylbenzyl)-N′-[4-(methylsulfonylamino)benzyl]thiourea analogues have been investigated as TRPV1 receptor antagonists. α-Methyl substituted analogues showed potent and stereospecific antagonism to the action of capsaicin on rat TRPV1 heterologously express...

In order to more rationally design thiourea-containing drugs and drug candidates, specifically thiourea-containing histamine H3 receptor antagonists, it is necessary to develop structure–toxicity relationships (STRs). For this purpose, the cytotoxicity of a series of thiourea-containing compoun...

As novel heat shock protein 70 (HSP70) inhibitors, N, N′-disubstituted thiourea derivatives were designed and synthesized based on the X-ray structure of the ATPase domain (nucleotide binding domain, NBD). An ATPase activity inhibition assay revealed that these compounds effectively inhibited H...

Two series of picolinamide derivatives bearing (thio)urea and dithiocarbamate moieties were designed and synthesized as VEGFR-2 kinase inhibitors. All the new compounds were screened for their cytotoxic activity against A549 cancer cell line and VEGFR-2 inhibitory activity. Compounds 7h, 9a and ...

An efficient one-pot four-component strategy involving aldehydes, amines, alkynes and isothiocyanates has been developed to access a novel series of thiazolidine-2-imines (5a-x). This process operates under the action of a cooperative catalysis composed of Cu(I) and Zn(II) delivering the desired...

Publisher SummaryLaboratory isotope separators originated from the principles of mass spectrometry and have reached a level of sophistication sufficient for separating stable isotopes for use in many experiments and for separating radioactive isotopes of very short duration. There is continuous ...

Patients affected by sulfite oxidase (SO) deficiency present severe seizures early in infancy and progressive neurological damage, as well as tissue accumulation of sulfite, thiosulfate and S-sulfocysteine. Since the pathomechanisms involved in the neuropathology of SO deficiency are still poorl...