The first method for the synthesis of the title compounds has been established involving a stereoselective electrochemical diacylation process. The cathodic reductions of monothiobenzils in an aprotic medium, under constant potential, in the presence of twofold molecular amounts of aroyl chlorid...
Sodium benzoate reacts with α-halo-α,β-enones in the presence of tetrabutylammonium hydrogensulfate or 18-Crown-6 to afford α- and/or γ-benzoyloxy-α,β-enones in good yield. The α/γ and γ/γ′ selectivities are dependent on the substrate and reagent.
Two new taxanes, named wallitaxane G (1) and H (2), were isolated from the roots of Taxus wallichiana (Taxaceae), together with nine known compounds (3−11). Their structures were elucidated on the basis of NMR spectroscopic analysis and the relative configurations of 1 and 2 were determined base...
An oxytocic antagonist, [1-(β-mercapto-β,β-cyclopentamethylenepropionic acid,2-O-methyltyrosine,4-threonine,8-ornithine, 9-tyrosylamide]vasotocin (d(CH2)5[Tyr(Me)2,Thr4,Tyr-NH29]OVT), was monoiodinated at the phenyl moiety of the tyrosylamide residue at position 9. 125I-labelling was performe...
SummaryThis paper describes the discovery of a new non-peptide endothelin A (ETA) selective ligand, 2,4-dibenzyloxybenzoic acid 3, which inhibits the binding of [125I]ET-1 to ETA receptors with an IC50 of 9 μM (ET-1 = endothelin-1). Optimisation of 3 resulted in compound 52 which had an IC50 of...
Three 4-isoxazolyl-3,5-disubstituted amidoximes have been obtained and several of their physicochemical properties have been studied. The pKa values have been potentiometrically determined, with each amidoxime having two protonation constants, one for low pH values (pKa 2.24–2.96), and one for ...
In the superbase KOH/H2O/toluene/phase-transfer catalyst system, 2-picolyl chloride, generated in situ from 2-(chloromethyl)pyridine hydrochloride, reacts with elemental phosphorus at 65–95 °C for 3 h to afford tris(2-picolyl)phosphine oxide in 50% yield. Single crystal X-ray analysis of the l...
The synthesis of 1-(4-nitrobenzyl)-2-chloromethyl benzimidazole, which undergoes a nucleophilic substitution with pyridine in the absence of additional base, is reported. The key steps are the reaction of 1,2-phenylenediamine to give exclusively the mono-substituted product and the avoidance of ...
The diarylisoxazole molecular scaffold is found in several NSAIDs, especially those with high selectivity for COX-1. Here, we have determined the structural basis for COX-1 binding to two diarylisoxazoles: mofezolac, which is polar and ionizable, and 3-(5-chlorofuran-2-yl)-5-methyl-4-phenylisoxa...
A series of 1-aryl-4-methyl-3,6-bis-(5-methylisoxazol-3-yl)-2-thioxo-2,3,6,10b-tetrahydro-1H-pyrimido[5,4-c]quinolin-5-ones (6a–h) have been synthesized by cyclization of ethyl-3-aryl-4-(2-chlorophenyl)-6-methyl-1-(5-methylisoxazol-3-yl)-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylates 4a–...
Some new thieno[2,3-d]pyrimidin-4(3H)-ones containing 1,2,4-triazole and 1,3,4-thiadiazole moiety were synthesized using thieno[2,3-d]pyrimidin-3(4H)-yl)acetohydrazides as precursors in order to determine their cytotoxicity. Compounds 5, 7–8 and 10–18 were evaluated for their cytotoxical effec...
A study was made of the electrophoretic behaviour of polyoxyethylene ethers of N-benzoylhistidine (POBH) with molecular weights of 15,000 and 40,000. It is shown that in both cases the polymer separates into two fractions: a mixture of monosubstituted POBH and unreacted polyoxyethylene (POE), of...
Metabotropic glutamate receptors (mGluR) are G-protein-coupled receptors that play a major role in modulatory pathways in the CNS and have been suggested to have pharmacological implications in pain, psychiatric disorders and other neurological states. 3-[(2-Methyl-1,3-thiazol-4-yl) ethynyl]-pyr...
The absolute configuration of 5-chloro-2-methoxy-N-phenylbenzamide single crystal [compound (1)] and the effect of introducing –[CH2]n–, n = 1,2 group adjacent to the amide group [compounds (2) and (3)], were studied. Furthermore, the replacement of the methoxy group with a hydroxy group [comp...
Glutamate intercalated Mg–Al layered double hydroxide (LDH) was prepared by co-precipitation and the removal of Pb2+ in the aqueous solution was investigated. The prepared samples were characterized by XRD, FT-IR and SEM. It was shown that glutamate can intercalate into the interlayer space of ...
The Co/Bi-layered double hydroxides (Co/Bi-LDH) were synthesized by co-precipitation method and used for the removal of lead from aqueous solutions. The Co/Bi-LDH was characterized using X-ray diffraction (XRD), Fourier Transform Infrared spectroscopy (FTIR), Transmission Electron Microscopy (TE...
This work prepared lanthanum hydroxide (La-OH) and magnetite/lanthanum hydroxide composite (Mag-La-OH), and then La-OH and Mag-La-OH were used as sediment amendments to immobilize phosphorus (P) in sediments. The immobilization efficiency of mobile P (MobP) and bioavailable P (BIO-P) in sediment...
IntroductionCalcium hydroxide (CH) and nano–calcium hydroxide (NCH) as intracanal medicaments may affect the physical and chemical properties of dentin. The aim of this investigation was to evaluate the effects of CH and NCH on the microhardness and superficial chemical structure of radicular d...
This study was performed in two phases of work. In the first stage, alkaline leaching of lead and zinc from an Iranian low-grade oxide ore was examined and the influence of the operating variables including stirring speed, leaching temperature, NaOH concentration and liquid to solid ratio was de...
Layered double hydroxides (LDH), also identified as anionic clays, have attracted much consideration due to their excellent ion exchange capacities, shape memory effect and ability to intercalate anions. LDH have been used in the different fields of applications such as biomedical, sensors and d...
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