In the present study, corn bran arabinoxylan (CAX) were modified with sinapic acid (SA) by esterification to generate sinapic acid corn bran arabinoxylan esters (SA-CAX) with various substituted degrees. The structure of SA-CAX was characterized by FT-IR, NMR and UV spectroscopy. And the antioxi...
A series of novel porphyrin-cinnamic acid (porphyrin/CA) conjugates (4a-4c) have been synthesized by condensation of 5-(4-Hydroxyphenyl)-10,15,20-triphenyl- porphyrin (1) with different substituted cinnamic acids (CAs) through an alkyl linker due to the biological activities of CAs and the appli...
Catechol esters of ortho-methoxyalkylphenylboronic acids have been synthesized and characterized by 17O NMR spectroscopy. The results were compared with the data for the parent acids. The influence of intramolecular and intermolecular hydrogen bonds on the properties of the boronic acids has bee...
The reaction of 3-(aryl)-2-sulfanylpropenoic acids [H2xspa; x: p = 3-phenyl-, f = 3-(2-furyl)-, t = 3-(2-thienyl)-] with methanol or ethanol gave the corresponding methyl (Hxspme) or ethyl (Hxspee) esters. The reaction of these esters (HL) with triphenyltin(IV) hydroxide gave compounds of the ty...
In this paper we report on the lipase-catalyzed preparation of enantiopure amines. Hydrolysis of two different (R,S)-[1-(4-chlorophenyl)] ethyl amides was best performed in phosphate buffer, resulting in conversions ∼48% and optical purities of the (S)-product >99% ee. Similar optical purities ...
A copper-catalyzed oxidative esterification of 2-carbonyl substituted phenols from the alcohol oxidation level is described. This protocol represents direct access to a range of 2-carbonylated aryl benzoate derivatives, which are important building blocks in the synthesis of natural and pharmaco...
A novel series of 4-anilinoquinazoline derivatives (19a–19t) were designed and synthesized through incorporation of the 2-nitroimidazole moiety into the 4-anilinoquinazoline scaffold of EGFR inhibitors. The most promising compound 19h displayed potent EGFR inhibitory activity with the IC50 valu...
Herpesviruses are a significant source of human disease; amongst these herpes simplex virus 1 (HSV-1) and HSV-2 are very prevalent and cause recurrent infections. We recently identified a pyrazolo[1,5-a]pyridine scaffold that showed promising activity against HSV-1 and HSV-2 in Vero cell antivir...
An efficient, mild, cost effective and practical method is presented for generation of esters (RCO2R′) from acids (RCO2H)/ 2-oxoacids (RCOCO2H)/ 2-oxoaldehydes (RCOCHO)/ 2-oxoesters (RCOCO2R″) and alcohols by using oxone as catalyst. In addition to deciphering the scope of our process, we prop...
N-((6,6-diphenyl-1,4-dioxan-2-yl)methyl)-2-(2-methoxyphenoxy)ethan-1-amine (3) is a potent 5-HT1A receptor and α1d-adrenoceptor (α1d-AR) ligand. Analogues 5–10 were rationally designed and prepared to evaluate whether electronic and/or lipophilic properties of substituents in the ortho positi...
A toxicological evaluation of a novel cooling agent, 2-(4-methylphenoxy)-N-(1H-pyrazol-3-yl)-N-(2-thienylmethyl) acetamide (S2227; CAS 1374760-95-8), was completed for the purpose of assessing its safety for use in food and beverage applications. S2227 undergoes rapid oxidative metabolism in vit...
The photochemical coupling of 5-oxazoylmethanol derivatives with benzophenone and benzaldehyde showed that the hydroxyl directing effect in the Paternò–Büchi reaction described in the case of allylic alcohols and furylmethanol derivatives can also be present in the case of 5-oxazolylmethanol ...
In this report we examined the presence of specific antibodies against equine herpesvirus type 1 (EHV-1), and equine herpesvirus type 4 (EHV-4) in several equidae, including mules, donkeys, horses. The presence of EHV-1 and EHV-4 in respiratory diseases of equids, and ability of multiplex nested...
Equid herpesvirus type 1 (EHV-1)-associated myeloencephalopathy (EHM) may follow an infection with the virus in horses. This study tested three hypotheses: (1) a large inhaled dose of a neuropathogenic EHV-1 strain would induce a cell-associated viraemia in all infected horses; (2) neurological ...
Five new diorganotin(IV) compounds were prepared by reacting diorganotin dichlorides R2SnCl2 (R = Me, nBu and Ph) with sodium salts of the tridentate NO2 ligands (E)-3-hydroxy-2-((2-hydroxybenzylidene)amino)propanoic acid (L1H2Na) and (E)-3-hydroxy-2-((1-(2-hydroxyphenyl)ethylidene)amino)propano...
The electrochemical behaviour of 2-(methylseleno)benzanilide, one of the major metabolites of Ebselen, together with a series of 2-methylseleno-(4′-X-phenyl)benzamides were investigated by voltammetry using a rotating platinum electrode, cyclic voltammetry, controlled potential coulometry and e...
The coupling reactions were performed using 3-ethoxy-4-iodo-5-methylisoxazole (4) as the key intermediate. Coupling of 4 under Suzuki–Miyaura or Stille conditions using Pd(PPh3)2Cl2 and arylboronic acids or aryltin analogues, respectively, gave 4-aryl substituted isoxazoles in yields ranging fr...
5-[3-(4-Arylpiperazin-1-yl)propyl]-1H-benzimidazoles and 5-[2-(4-arylpiperazin-1-yl)ethoxy]-1H-benzimidazoles were synthesized and their affinity for the D1, D2 and 5-HT1A receptors examined. They expressed a rather high affinity for the D2 dopamine receptor. The main features of ligand–D2 rece...
New C2-symmetric and C2-asymmetric Co-Schiff base catalysts tethered to arylpiperazine units were synthesized and used to oxidize phenolic lignin models to para-benzoquinones. Synthetic approaches to these catalysts were optimized to include fewer steps and broaden the types of catalyst structur...
Impedance Spectroscopy (IS) and Differential Scanning Calorimetry (DSC) measurements, which we have performed at different concentrations and temperatures, support a peculiar order-disorder transition model for lithium perchlorate dissolved in Poly(ethylene glycol-400) distearate systems (LiClO4...
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