We aimed to investigate the local anesthetic effect of 2-adamantanamine in spinal anesthesia. The dose–response curves were constructed after intrathecally injecting the rats with five doses of 2-adamantanamine and a common local anesthetic mepivacaine. The quality and duration of 2-adamantanam...

Indium(III) chloride was found to be an efficient catalyst for the synthesis of 3-(5-amino-1H-pyrazol-4-yl)-3-(2-hydroxy-4,4-dimethyl-6-oxocyclohex-1-enyl)indolin-2-ones by one-pot, three-component reaction of dimedone, 1H-pyrazol-5-amines and isatins in water under ultrasonic irradiation. The a...

Screening a 3-aminopyridin-2-one based fragment library against a 26-kinase panel representative of the human kinome identified 3-amino-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2(1H)-one (2) and 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one (3) as ligand efficient inhibitors of the mitotic kinase Monopol...

The reaction of 2-(5-amino-4-carbamoyl-1-methyl-1H-pyrazol-3-yl)acetic acid and triethylorthoformate did not give the expected dihydropyrazolo[4,3-c]pyridin-4-one product as described in literature, but formed an alternative cyclic imide product, fully characterised by NMR and X-ray crystallogra...

Sodium acetate-catalyzed multicomponent reaction of salicylaldehydes, malononitrile and 3-methyl-2-pyrazolin-5-one initiated by grinding in mortar in the presence of small quantities of water results in the fast (10 min) and efficient formation of substituted 2-amino-4-(1H-pyrazol-4-yl)-4H-chrom...

Through virtual screening, we identified the lead compound MCL1020, which exhibited modest CHK1 inhibitory activity. Then a series of 5-(pyrimidin-2-ylamino)picolinonitrile derivatives as CHK1 inhibitors were discovered by further rational optimization. One promising molecule, (R)-17, whose pote...

Asymmetric “allyl”boration of pentafluorobenzaldehyde with various α-pinene based “allyl”boranes provides homoallylic alcohols in high de and ee; the alcohols have been converted into δ-lactones via acryloylation, ring-closing metathesis and hydrogenation. Pentafluorophenyl analog of key p...

A pseudo template molecularly imprinted polymer (MIP) for selective extraction of β-agonists was prepared using 4-hydroxyphenethyl alcohol as pseudo template molecule, methyl acrylic acid as functional monomer, and ethylene glycol dimethacrylate as cross-linker. Selectivity and adsorption capac...

The menopausal period, an inevitable physiological process for women, is frequently associated with physiological and psychological dysfunction attributable to substantial fluctuation and gradual decrease in female hormones induced by ovarian failure, leading to corresponding symptoms and diseas...

Five spectrophotometric methods were successfully developed and validated for the determination of betamethasone valerate and fusidic acid in their binary mixture. Those methods are isoabsorptive point method combined with the first derivative (ISO Point – D1) and the recently developed and wel...

SummaryIntroduction and objectivesThe desire to preserve the prepuce is often based on cultural norms. Recently, the concept of “genital autonomy” has been invoked to delay circumcision (or any genital altering procedure) until the individual reaches maturity and can make his or her own decisi...

The aim of this study was to target a naturally chemotherapeutic agent: ferulic acid to the liver using a biocompatible and an in vivo stable carrier. Accordingly, chitosan as a biopolymer was modified using a hydrophobic moiety and valeric acid in order to increase its in vivo stability. The st...

The thermal decomposition of barium valerate (Ba(C4H9CO2)2/Ba-pentanoate) was studied in argon by means of thermogravimetry, differential thermal analysis, IR-spectroscopy, X-ray diffraction and hot-stage optical microscopy. Melting takes place in two different steps, at 200 °C and 280 °C and ...

A series of novel aliphatic copolyesters bearing vinylsulfide and ketone functional groups were synthesized via lipase catalyzed polycondensation of vegetable oil derivatives. The vinylsulfide-containing hydroxyacid (VSHA) from 10-undecenoic fatty acid and the ketone-containing hydroxyester (KHE...

Two enantiomeric pairs of menthol derivatives, the menthol ester with 10-undecynoic acid and the 2-tricyanovinyl-pyrrole derivative of the methoxy-menthol, have been synthesized and their pure enantiomers obtained. The X-ray crystal and molecular structure of the (+)-enantiomer of the latter com...

By adaptation of a literature method developed in the glucose series and standard protecting group manipulations a 2-deoxy-d-glucose derivative is converted to a series of 1R,2R,5R-3-hydroxymethyl-cyclohexen-1,2,5-triol derivatives whose reduction to the corresponding diastereomeric d-gluco and ...

The N-hydroxymethyl derivatives of α-amino aldehydes 1 were utilized for the effective synthesis of several β-amino-α-hydroxy acid derivatives in a one-pot process starting from the corresponding α-amino aldehydes. Properly protected methyl esters 3 were prepared in 65–79% yields from α-am...

Hearing loss is a significant public health problem, and the “loss of sensory hair cells” is one of two leading causes in humans. Advanced imaging reagents are desirable for understanding the role of the surrounding support cells in the loss or regeneration of the hair cells. A styryl dye was ...

A series of six aromatic esters of both 5‐dimethyl‐amino‐1‐phenyl‐3‐pentanol and 3‐dimethylamino‐1‐(2‐phenylcy‐clohexyl)‐1‐propanol was prepared. Antimicrobial evaluation showed that the cyclic analogs had approximately twice the activity of the open chain series; in particular, the...

Copper(II) complexes with glycyl-dl-α-amino-n-butyric acid (H2gly-dl-but), glycyl-dl-valine (H2gly-dl-val), glycyl-dl-norleucine (H2gly-dl-norleu), glycyl-dl-threonine (H2gly-dl-thr), glycyl-dl-serine (H2gly-dl-ser), glycyl-dl-phenylalanine (H2gly-dl-phe), and glycyl-l-valine (H2gly-l-val), hav...