Ring opening of protected 3-aminoalkyl-substituted azetidin-2-ones with O-, N- or S-nucleophiles led to β,β′-diaminocarboxylic esters, amides and thioesters, respectively. The reaction outcome is improved by the addition of catalytic amounts of sodium azide. Utilization of a glycine derivativ...

Derivatives of 7-amino-6-azaindole containing variable substituent in the amino group were synthesized via acid-catalyzed nucleophilic heteroaromatic substitution (SNHetarH+) using 7-chloro-6-azaindoles as substrates and aliphatic and aromatic amines as nucleophiles. The protonation of the pyrid...

A series of 4-amino-5-vinyl-3(2H)-pyridazinones and analogues were synthesized and their antinociceptive effect was evaluated in the mouse abdominal constriction model. Several of the novel compounds showed ED50 values in the range 6–20 mg/kg/sc and demonstrated to be able to completely protect...

Dihydroxylation of 6-vinylpurines with t-BuOOH and OsO4 gave 6-(1,2-dihydroxyethyl)purines 2, while the epoxidation with H2WO4 and t-BuOOH afforded 6-(oxiran-2-yl)purines 3. Oxirane ring-opening reactions of 3 with diverse nucleophiles gave a series of title 6-(1,2-disubstituted ethyl)purine bas...

A novel series of 2-amino-1,3,5-triazines bearing a tricyclic moiety as heat shock protein 90 (Hsp90) inhibitors is described. Molecular design was performed using X-ray cocrystal structures of the lead compound CH5015765 and natural Hsp90 inhibitor geldanamycin with Hsp90. We optimized affinity...

Signal transducers and activators of transcription 6 (STAT6) is a key regulator of the type 2 helper T (Th2) cell immune response and a potential therapeutic target for allergic diseases such as asthma and atopic diseases. To search for potent and orally bioavailable STAT6 inhibitors, we synthes...

Synthetically feasible and cost effective Ni(II) complex phosphor (4) as green organic light emitting diode (OLED) was prepared by using Schiff base 1-[(4-butylphenyl)imino]methyl naphthalen-2-ol (3). The single crystals of Ni(II) complex were grown from chloroform and hexane (1:1 v/v) solution....

Organic light-emitting devices (OLEDs) with a poly(N,N′-bis-4-butylphenyl-N,N′-bisphenyl)benzidine (poly-TPD):octadecylamine (ODA)-graphene quantum dots (GQDs) hole transport layer (HTL) were fabricated to enhance their efficiency. Photoluminescence (PL) and PL excitation spectra showed that t...

N-benzoate alkylamines were used as the aminating agents, a efficient Rh-catalyzed ortho CH amination of 2-arylquinazolin-4(3H)-one has been reported. The reactions exhibit high efficient and good functional group tolerance. Exclusive 2,6-bis-aminated product and good to excellent yields were ob...

The reaction of bis(2-bromoethyl)selenium dibromide (1a) with 1,5-hexadiene (2) in methanol or ethanol affords 2,5-bis(alkoxymethyl)tetrahydroselenophene-1,1-dibromides (R  CH3 (3b), R  C2H5 (3c)) via 2,5-bis(bromomethyl)tetrahydroselenophene-1,1-dibromide (3a). The reaction of 1a with 2 in ...

Quantum mechanical calculations of energies, geometries, and vibrational wavenumbers of N-(bromomethyl)phthalimide and N-(chloromethyl)phthalimide are carried out using density functional theory (DFT/B3LYP) method with 6-31G and 6-311G(d,p) basis sets. The optimized geometrical parameters obtain...

The steroid 17-PA is a GABAA receptor antagonist which is finding use as a tool in evaluating agonistic/antagonistic activity at GABAA receptors. Compounds with improved efficacy over 17-PA would be are advantageous for such studies. Accordingly a series of novel analogues of the neurosteroid 17...

Human sirtuin 2 (SIRT2) is an attractive target molecule for development of drugs to treat neurodegenerative diseases and cancer, because SIRT2 inhibitors have a protective effect against neurodegeneration and an anti-proliferative effect on cancer stem cells. We designed and synthesized a serie...

Algae are known for high ash content. It is important to properly characterize their ash for value added utilization of algae as food, feed, and feedstock for biofuels. In this study, 12 algae of different sources were measured for proximate composition and mineral profile. Results showed that t...

This paper presents the effects of some admixtures including silica nanoparticles, silica fume and Class F fly ash on different properties of high performance self compacting concrete (HPSCC). For this purpose, a fraction of Portland cement with the aim of cement content reduction was replaced d...

Airborne lead and acidic gasses are generated through combustion and mechanical abrasion of ammunition constituents during shooting events. Shooters and other personnel at shooting ranges are exposed to these airborne toxicants and the potential health risks of irritation, nervous system damage,...

Silica layers fabricated by the sol-gel method are usually amorphous and exhibit a relatively low refractive index (n∼1.46 at about 0.6 μm), high optical transmittances at UV-VIS and near-IR ranges, as well as high thermal stability. Such layers can be used as high reflection or antireflection...

1-Aminoethyl-3-arylsulfonyl-1H-indoles 1 are 5-HT6 receptor ligands with modest activity in a 5-HT6 cyclase assay. Introduction of an additional nitrogen in the indole ring provides 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines 2 with both enhanced 5-HT6 affinity and cyclase activity, m...

An efficient route to novel 4,7-dihydro-1H-pyrrolo[2,3-b]pyridines with incorporated tetrahedral fragment in the position-4 via three-component reaction of N-substituted 5-amino-3-cyanopyrroles, various carbonyl and active methylene compounds has been developed. In the same time, by using develo...

Four series of phenylpicolinamide derivatives bearing 1H-pyrrolo[2,3-b]pyridine moiety (12a–e, 13a–f, 14a–f and 15a–i) were designed, synthesized and evaluated for the IC50 values against three cancer cell lines (A549, PC-3 and MCF-7) and c-Met kinase. Five selected compounds (13b, 15b, 15d,...