β-Secretase (BACE1) has been widely recognized as one of the possible therapeutic targets for the treatment of Alzheimer’s disease. In this paper, we report the synthesis and the BACE1 inhibitory activity of new, variously substituted N-(3-(4-benzhydrylpiperazin-1-yl)-2-hydroxypropyl) arylsulf...

Synthesis of C-5-substituted 1,3-dioxoisoindoline-4-aminoquinolines having amide group as a spacer was developed with an intent to evaluate their antiplasmodial activities. The synthesized dioxoisoindoline-aminoquinolines tethered with β-alanine as a spacer and secondary amine as substituent di...

The reference standard N-(4-diethylamino)benzyl-4-methoxy-N-(p-tolyl)benzenesulfonamide (3c) (CB2, Ki=0.5 nM; CB1, Ki=1297 nM; selectivity CB1/CB2=2594) and its corresponding precursor N-(4-diethylamino)benzyl-4-hydroxy-N-(p-tolyl)benzenesulfonamide (3d) were synthesized from 4-(diethylamino)ben...

New subphthalocyanines were synthesized by threatening 2-[4-({(1E)-[4-(dimethylamino)phenyl]methylene}amino)phenyl]ethanol 2 and 2-[4-({(1E)-[4-(diethylamino)phenyl]methylene}amino)phenyl]ethanol 3 with excess of boron subphthalocyanine chloride in toluene. The subphthalocyanines containing 2-[4...

Phosphoenolpyruvic acid crystals, obtained by slow concentration of an aqueous solution, are triclinic, space group P1, with a = 5.905(5), b = 8.135(8), c = 14.095(15) Å, α = 104.70(8), β = 97.72(8), γ = 100.99(8)°, and Z = 4. Two crystallographically independent phosphoenolpyruvic acid mole...

Reaction of 1-methyl-8-amino-3,13,16-trithia-6,10,19-triazabicyclo[6.6.6]icosane (AMN3S3sar) with the amide coupling agent 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium chloride (DMT-MM) and 4-nitrobenzoic acid, the protected amine 4-(1,3-dioxoisoindolin-2-yl)benzoic acid and the tri...

(Bio)degradable poly(ester-urethane)s containing polylactide (PLA) and poly[(1,4-butylene terephthalate)-co-(1,4-butylene adipate)] (BTA) segments in the main chain were synthesized and their properties were examined. Novel poly(ester-urethane)s were obtained from isophorone diisocyanate (IPDI),...

A series of novel methyl cellulose (MC) composite films were prepared using polyethyleneimine reduced graphene oxide (PEI-RGO) as an effective filler for water vapor barrier application. The as-prepared PEI-RGO/MC composites were characterized by Fourier transform infrared spectroscopy, X-ray di...

Low molecular weight products migrating from linear and branched poly(butylene adipate) (PBA) and poly(butylene succinate) (PBS) during hydrolysis were extracted, identified and quantified by solid phase extraction (SPE) and GC–MS. The combination of SPE and GC–MS proved to be a sensitive tool...

This work investigates the feasibility of using coffee silverskin (CSS), one of the most abundant coffee waste products, as a reinforcing agent in biopolymer based composites. The chemical composition, antioxidant activity and morphology of CSS were studied by specific chemical essays and scanni...

Polyesteramide multiblock copolymers based on polyamide 6 and diepoxy propylene adipate blocks were synthesized. For this purpose a carboxyl-terminated polyamide 6 (Mn = 2400 g/mol, Tm = 205.5 °C) and diepoxy propylene adipate (Mn = 450 g/mol) were separately synthesized and characterized. The ...

The synthesis and the properties of the first polymerised High Internal Phase Emulsions (polyHIPEs) derived from co-reacted tannin and furfuryl alcohol resin, are reported in this paper. Such highly porous thermoset polymers were obtained by emulsion-templating in the form of strong monoliths, u...

This paper gives detailed insight in the solventless synthesis of (meth)acrylate esters catalysed by Novozym 435 with a focus on the quantitative understanding of the reaction kinetics. The (meth)acrylate esters were formed from various (heavy boiling) alcohols by applying methyl (meth)acrylate ...

The unperturbed dimensions of isotactic, optically active poly-(S)-4-methyl-1-hexene and isotactic poly-4-methyl-1-pentene were estimated from viscosity data. The characteristic ratio h02/nl2 for the optically active polymer is remarkably higher than that of the structurally analogous poly-4-met...

The BF3-catalyzed cyclization of 3-acetyl-1-aryl-2-pentene-1,4-diones 1a–e in the presence of water in boiling tetrahydrofuran gave bis(3-acetyl-5-aryl-2-furyl)methanes 2a–e in 26–79% yields along with a small amount of 3-acetyl-5-aryl-2-methylfurans 3a–e. The exact structure of 2a was deter...

The decompositions of the following poly(vinyl chloride) models were investigated in the gas phase: trans-1,3-dichloro-1-pentene (in the range 310–380°), trans-5-chloro-3-heptene (296–357°), cis-4-chloro-2-pentene (295–340°) and racem, and meso 2,4-dichloropentane at 351 and 370°. The dec...

In situ generated [{Ru(P(OCH3)3)2(CH3CN)3}2(μ-S2)]4+ (2), produced by abstracting the chloride atoms from [{Ru(P(OCH3)3)2Cl}2(μ-Cl)2(μ-S2)] (1) with Ag+ salts, reacts with 1-pentene in CH3CN to afford [{Ru(P(OCH3)3)2(CH3CN)3}2{μ-SCH2CHC(CH3)CH2S}]4+ (4) via dehydroisomerization of 1-pentene,...

A unique photoreaction of methyl 6-chloro-3,4-dihydro-4-methyl-3-oxo-2H-1,4-benzoxazine-8-carboxylate in methanol gives four β -lactam compounds, methyl 6-chloro-2,9-dioxo-1-methyl-1-azaspiro[3.5]nona-5,7-diene-8-carboxylate and three stereoisomers of dimethyl 3-chloro-4-(1′-methyl-2′-oxoazet...

1-Chloro-2-hydroxy-3-butene (CHB) is an in vitro metabolite of 1,3-butadiene, a rodent/human carcinogen. To search for an approach detecting CHB in vivo, it is vital to obtain a full understanding of CHB metabolism. Previously, we demonstrated that CHB was bioactivated to 1-chloro-3-buten-2-one ...

Rimantadine HCl was assessed for its effect on influenza A virus titer in lungs of infected BALB/c mice. Rimantadine administered orally via drinking water, with and without an intraperitoneal prophylactic loading dose, was compared to intraperitoneal administration. Mice were infected with a no...