The preparation and preliminary evaluation of 2, an analog of sandramycin, are detailed. Although 2 was typically 4–10x less potent than sandramycin against leukemia cell lines, it was found to be 1–10,000x more potent against melanomas, carcinomas, and adenocarcinomas exhibiting typical IC50 ...

The gastrointestinal hormone cholecystokinin (CCK) regulates digestive processes and satiety in addition to centrally mediated effects on nociception and anxiety. CCK signals through two seven-trans-membrane receptors named the CCK-1 receptor and the CCK-2 receptor. The expression pattern and bi...

New, flexible (7, 9, 11 and 13) and rigid (8, 10, 12 and 14) imides with a 1-(m-trifluorophenyl)piperazine fragment and a tetramethylene or a 1e,4e-cyclohexylene spacer, respectively, showed very high affinity (Ki = 0.3–34 nM) and agonistic in vivo activity for 5-HT1A receptors. Flexible new co...

The present study examined the roles of ventrolateral orbital cortex (VLO) 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HT5, 5-HT6 and 5-HT7 receptor subtypes in mediating 5-HT-induced antiallodynic actions in the rat spared nerve injury (SNI) pain model. Changes in paw withdrawal threshold (PWT) were measured...

Starting with the structure of potent 5-HT1A ligands, that is, MM77 [1-(2-methoxyphenyl)-4-(4-succinimidobutyl)piperazine, 4] and its constrained version 5 (MP349), previously obtained in our laboratory, a series of their direct analogues with differently substituted aromatic ring (R = H, m-Cl, ...

The crystal structures of cis and trans-isomers of 2-{4-[4-(2-methoxyphenyl)piperazin-1-yl]but-2-enyl}isoindoline-1,3-diones have been solved in two different forms – as free bases and as hydrochlorides. It was concluded that the conformations of arylpiperazine derivatives with an aliphatic spa...

AimsOur study focuses on the design and synthesis of a new piperazinic derivate, 4-(1-phenyl-1h-Pyrazol-4-Ylmethyl)-Piperazine-1-Carboxylic Acid Ethyl ester (LQFM008), and evaluation of its anxiolytic-like profile in Swiss mice.

In the search for a novel serotonin 7 (5-HT7) receptor PET radioligand we synthesized and evaluated a new series of biphenylpiperazine derivatives in vitro. Among the studied compounds, (R)-1-[4-[2-(4-methoxyphenyl)phenyl]piperazin-1-yl]-3-(2-pyrazinyloxy)-2-propanol ((R)-16), showed the best co...

Piperazine compounds possess anti-infective, anti-carcinogenic, anxiolytic, hypotensive, anti-hypertensive and vasorelaxant properties and are attractive candidates for the development of new analgesic and anti-inflammatory drugs. This study investigates the anti-nociceptive and anti-inflammator...

Synthesis, spectral and single crystal XRD studies of a novel ligand 1-phenyl-3-methyl-4-benzoyl-5-pyrazolone N(4)-methyl-N(4)-phenylthiosemicarbazone and its cadmium(II) complex have been communicated in this work. The ligand crystallizes in triclinic system with space group P-1, a(Å) = 7.8930(...

Thioureas are important sulfur and nitrogen containing compounds and they are useful substances in drug research. In an effort to improve potential anticancer activities, two novel 1-benzoyl-3-methyl thiourea derivatives were designed and synthesized with substitution at aromatic positions of C-...

Three new complexes [H2en][Ni(pchc)2] (1) (pchc = pyridine-4-carbonyl-hydrazine carbodithioate), [Ni(Hppith)2] (2) (H2ppith = 1-phenyl-3-pyridin-2-yl-isothiourea) and [Ni(mppcdt)2] (3) {mppcdt = 4-(2-methoxyphenyl)piperazine-1-carbodithioate} have been synthesized and characterized by elemental ...

Two amphetamine-like piperazine-containing compounds, 1-(3,4-methylenedioxyphenyl)-2-piperazinopropane (3,4-MDPPP), its positional isomer 1-(2,3-methylenedioxyphenyl)-2-piperazinopropane (2,3-MDPPP) and three methcathinone-like piperazine-containing regioisomeric ring substituted 1-(methoxypheny...

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 ...

Antagonists addressing selectively NMDA receptors containing the GluN2B subunit are of particular interest for the treatment of various neurological disorders including neurodegenerative diseases. With the aim to bioisosterically replace the metabolically labile phenol of 7-amino-6,7,8,9-tetrahy...

Novel bis(hydroxymethyl) alkanoate curcuminoid derivatives were designed, synthesized and screened for in vitro antiproliferative and in vivo antitumor activity. Selected new compound 9a and curcumin were further evaluated for inhibitory activity against ER+/PR+ breast cancer (MCF-7, T47D), HER ...

Publisher SummaryThere are three specific inhibitors currently used in experiments on adenine nucleotide transport—namely, atractyloside (or atractylate) (ATR), carboxyatractyloside (C-ATR), and bongkrekic acid (BA), were originally found to be linked to human intoxication. The former two inhib...

Atractyloside (20 μm) has been found to decrease the incorporation of dATP-3H into DNA by 90% in intact mitochondria (at a level of 3 mg of protein) but to have no such effect on sonic extracts of mitochondria nor on the DNA polymerase from Escherichia coli. Inhibition of dATP-3H incorporation ...

Atractyloside (ATR) is widely used as a specific inhibitor of mitochondrial adenine nucleotide translocase and it is also a potent nephrotoxin that selectively injures the proximal tubule in vivo. This regioselectivity has been attributed to the prominence of mitochondria in the proximal tubule ...

Acute extrarenal and renal changes were noted following the intravenous administration of atractyloside (ATR) (12.97 and 32.40 μmol/kg) to spontaneously-respiring pentobarbital-anesthetized dogs. Severe hypoglycemia, respiratory depression and hypoxemia developed within 2 h. These extrarenal ch...