Novel compounds bearing a joint thiazole and a Z-5-aminopent-3-enoic acid fragments have been synthesized from readily accessible 5-bromolevulinic esters through a sequence of nucleophilic substitution, bromination, Hantzsch-type heterocyclization and Gabriel-like deprotection reactions. A major...

Hsp90 is a molecular chaperone that heals diverse array of biomolecules ranging from multiple oncogenic proteins to the ones responsible for development of resistance to chemotherapeutic agents. Moreover they are over-expressed in cancer cells as a complex with co-chaperones and under-expressed ...

The present study assessed the biological potential of fourteen 1,3-thiazolidin-4-ones evaluating the antiglioma effect through decreasing of cell viability of glioblastoma multiform cells. The new compounds were efficient synthesized through multicomponent or multicomponent one-pot procedures i...

Easily accessible 2-substituted 4-aryl-5-methoxy- and 2-substituted 5-aryl-4-methoxypyridazin-3(2H)-ones were transformed into the corresponding aryl-hydroxypyridazin-3(2H)-ones by alkaline hydrolysis. The use of these compounds in the synthesis of 2-substituted 4,5-diarylpyridazin-3(2H)-ones wi...

PurposeIn vivo imaging of GABAA receptors is essential for the comprehension of psychiatric disorders in which the GABAergic system is implicated. Small animal SPECT provides a modality for in vivo imaging of the GABAergic system in rodents using [123I]Iomazenil, an antagonist of the GABAA recep...

SummaryTo investigate involvement of extrafocal regions in mesial temporal lobe epilepsy (MTLE), we retrospectively explored abnormalities in distribution of iomazenil (IMZ) activity by identifying interhemispheric asymmetry on IMZ-SPECT images of patients with MTLE. Fourteen MTLE patients in wh...

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 first synthesis of (7S,9R)-decarestrictine H and (7R,9R)-decarestrictine H as well as the improved synthesis of decarestrictine J were achieved. The overall yields of (7S,9R)-decarestrictines H and J were 20.9% each in nine to ten steps from (R)-Roche ester using a unified synthetic route vi...

A facile chiral pool total synthesis of 9-epi-decarestrictine-D, decarestrictine-D and O has been achieved from l-(+)-diethyl tartrate. The strategy utilized is conventional and flexible. Wittig homologation and Grubbs ring closing metathesis are the key reactions employed for the synthesis of t...

Biochar addition to agricultural soils might increase the sorption of herbicides, and therefore, affect other sorption-related processes such as leaching, dissipation and toxicity for plants. In this study, the impact of wheat straw biochar on the sorption, leaching and dissipation in a soil, an...

The direct enantiomeric resolution of the racemic herbicide 2-(4-chloro-2-methylphenoxy)propanoic acid (CMPP) was demonstrated on an Enantiopac (α1-acid glycoprotein) chiral high-performance liquid chromatographic (HPLC) column. The HPLC separation of various amide derivatives of CMPP on a chir...

The photocatalytic decomposition of the herbicide (4-chloro-2-methylphenoxy)acetic acid (MCPA), C9H9ClO3, in aqueous suspensions containing TiO2 was investigated by following the formation of intermediates via recording proton NMR spectra. One of theoretically possible intermediates, 4-chloro-2-...

The work describes a study of the oxidation power of nitrogen-doped titanium dioxide (TiO2) suspensions for photocatalytic degradation of the herbicides RS-2-(4-chloro-o-tolyloxy)propionic acid (mecoprop) and (4-chloro-2-methylphenoxy)acetic acid (MCPA) using various light sources. The nitrogen-...

We have investigated the role of nitric oxide (NO) in relaxations to β-adrenoceptor agonists in mesenteric artery from wild-type (WT) and NO synthase-3 knockout (NOS-3-KO) mice. Isoprenaline, formoterol and BRL 37344 ((R⁎,R⁎)-(±)-4-[2-[(2-(3-chlorophenyl)-2-hydroxyethyl)amino]propyl]phenoxyace...

1-(4′-Ethylphenoxy)-3,7-dimethyl-7-methoxy or ethoxy-trans-2-octene (the ethyl-methoxide and ethyl-ethoxide) are more stable in some biological systems and less stable in others than 1-(4′-ethylphenoxy)-3,7-dimethyl-6,7-epoxy-trans-2-octene (the ethyl-epoxide). In housefly adults and mealworm ...

The metabolism of R-20458 [(E)-6,7-epoxy-1-(4-ethylphenoxy)-3,7-dimethyl-2-octene] by rat hepatocytes has been analyzed and compared with that of juvenile hormone I [methyl-(E,E)-cis-10,11-epoxy-7-ethyl-3,11-dimethyl-2,6-tridecadienoate] under identical conditions. The metabolism of R-20458 is c...

An I2-mediated protocol was proposed for the synthesis of 3-phenoxy imidazo heterocycles from aromatic ketones and 2-aminopyridines or 2-aminobenzothiazole. This direct, efficient and operationally simple method provided a fundamentally novel and rapid approach for the synthesis of 3-phenoxy imi...

Racemic 3-(2-ethylphenoxy)propane-1,2-diol 2 has been effectively resolved into (S)- and (R)-enantiomers by a preferential crystallization procedure. Non-racemic diols 2, obtained via a Mitsunobu reaction, have been converted into the non-racemic 1,2-epoxy-3-(2-ethylphenoxy)propanes (S)- and (R)...

Insect growth regulators (IGRs) are attractive pest control agents due to their high target specificity and relative safety to the environment. Recently, plants have been shown to synthesize IGRs that affect the insect juvenile hormone (JH) as a part of their defense mechanisms. Using a yeast tw...

Potato (Solanum tuberosum) is a major food crop, while the most tissues of potato accumulates steroidal glycoalkaloids (SGAs) α-solanine and α-chaconine. Since SGAs confer a bitter taste on human and show the toxicity against various organisms, reducing the SGA content in the tubers is requisi...