A new class of corticotropin releasing factor 1 (CRF1) receptor antagonists characterized by a tricyclic core ring was designed and synthesized. Novel tricyclic derivatives 2a–e were designed as CRF1 receptor antagonists based on conformation analysis of our original 2-anilinobenzimidazole CRF1...

The vaporization enthalpies and vapor pressures of three major components in ginger, α-zingiberene, β-sesquiphellandrene, and (−) ar-curcumene are evaluated by correlation gas chromatography using two set of standards, n-alkanes and a series of cyclic and polycyclic hydrocarbons. Vaporization ...

The equilibrium structures of 1H-, 2H-, and 3H-diazaphospholes and the 2-formyl and 4-amino derivatives of the 2H-isomer have been evaluated by ab initio gradient computation at the Hartree—Fock level. Split valence shell basis sets were used with d functions on the phosphorus atom and with add...

An efficient and mild protocol has been developed for the Minisci acylation reactions of nitrogen-containing heteroarenes with α-keto acids. Distinct from the conventional Minisci acylation conditions, the chemistry was performed using non-noble metal Fe(II), instead of expensive Ag(I) salt, as...

We describe the design, synthesis, and physicochemical and biological properties of a novel series of 7-heterocycle-6-trifluoromethyl-3-oxoquinoxaline-2-carboxylic acids bearing a substituted phenyl group joined through a urethane or urea linkage to the heterocycle at the 7 position. Introductio...

Ca2+-entry via L-type Ca2+ channels (DHPR) is known to trigger ryanodine receptor (RyR)-mediated Ca2+-release from sarcoplasmic reticulum (SR). The mechanism that terminates SR Ca2+ release is still unknown. Previous reports showed evidence of Ca2+-entry independent inhibition of Ca2+ sparks by ...

We have investigated the effects of imperatoxin A (IpTxa) on local calcium release events in permeabilized frog skeletal muscle fibers, using laser scanning confocal microscopy in linescan mode. IpTxa induced the appearance of Ca2+ release events from the sarcoplasmic reticulum that are ∼2 s an...

Three 6-substituted 3-chloropyridazine derivatives were tested for their potentials to protect mild steel surface and inhibit mild steel corrosion in 1 M HCl solution. The compounds are 3-chloro-6-(1H-pyrazol-1-yl)pyridazine (Pz1), 1-(6-chloropyridazin-3-yl)piperidin-4-ol (Pz2), and 3-chloro-6-(...

A new series of pyrazole-containing s-triazine derivatives were synthesized by reaction of the corresponding s-triazinyl hydrazine derivatives with acetylacetone in the presence of HClO4 or DMF/TEA. The former method allowed the preparation of the target products with higher yields. All compound...

Breast cancer remains a significant health problem due to the involvement of multiple aberrant and redundant signaling pathways in tumorigenesis and the development of resistance to the existing therapeutic agents. Therefore, the search for novel chemotherapeutic agents for effective management ...

The present study deals with the efficient chemo-enzymatic synthesis of enantiopure (R)-1-chloro-3-(piperidin-1-yl) propan-2-ol 3, as an intermediate for (R)-arimoclomol. This intermediate was synthesized from racemic alcohol (RS)-3 using lipases with vinylacetate as the acyl donor in three diff...

New polyimide–silica hybrid materials were prepared using the polyamic acid synthesized by copolymerization of 3,3′,4,4′-benzophenonetetracarboxylic dianhydride (BTDA), 4,4′-oxydianiline (ODA) and an A2A′-type tri-functional amine, 1,1-bis(4-(aminophenoxy)phenyl)-1-(4-(4-amino-2-trifluorome...

A series of novel bisquinoline derivatives connected by a 4-oxy-3-fluoroaniline moiety were synthesized and evaluated for their in vitro antitumour activities against a panel of five cancer cell lines (H460, HT-29, MKN-45, U87MG, and SMMC-7721). Most of compounds tested showed a potent activity ...

New 2-(4-(2-(dimethylamino)ethyl)-4H-1,2,4-triazol-3-yl)pyridine derivatives were synthesized and evaluated for their in vitro cytotoxicity against five cancer cell lines namely MKN-45, H460, HT-29, A549 and U87MG, as well as the normal cell line WI-38. Nearly all the compounds exhibited superio...

Deregulation of receptor tyrosine kinase c-Met has been reported in human cancers and is considered as an attractive target for small molecule drug discovery. In this study, a series of 4-phenoxyquinoline derivatives bearing sulfonylurea moiety were designed, synthesized and evaluated for their ...

The multiple reactivity of the mesomeric anion formed by N- or C(3)-deprotonation of 3-unsubstituted oxindoles hampers the selective introduction of substituents onto the nitrogen atom. A conveniently applicable reaction sequence has been elaborated for the synthesis of 3-unsubstituted oxindole-...

A synthetic procedure, for the synthesis of a series of functionalized benzofurans 3–5 and benzonaphthofurans 6, starting from intermolecular O-alkylation of α-bromoaryl ketones 2 with potassium oxygenated phenoxides 1 followed by Ga(OTf)3-catalyzed direct intramolecular cyclodehydration of th...

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...

With the emerging technology and consumption modes under “Big data” context, e-commerce has arisen as a new trend for e-waste recycling. This paper conducted a questionnaire survey from 896 residents living in the cities of China, to explore the development of e-commerce in e-waste recycling. ...

This special issue of Learning and Instruction examines the role of emotions in academic learning, with a special focus on emotions in computer-supported academic learning (or e-learning). Three central research challenges concerning emotion in e-learning are: identification (e.g., what are the ...