On the basis of previous reports on the importance of thienyl, furyl or phenol group substitution on 5H-indeno[1,2-b]pyridine skeleton, a new series of rigid 2-aryl-4-(4′-hydroxyphenyl)-5H-indeno[1,2-b]pyridine derivatives were systematically designed and synthesized. Topoisomerase inhibitory a...
Complexes of Tb(III) with the biscoumarin derivative 3,3′-[(4-hydroxyphenyl)methyl]bis-(4-hydroxy-2H-chromen-2-one) are synthesized by using a solution of tetraethylammonium hydroxide, [(C2H5)4N]OH, in water as deprotonating base. Elemental analysis, IR- and fluorescence spectroscopy are used t...
A simple three-step synthesis of 5-(3-hydroxyphenyl)-2-methyl-2-azabicyclo[3.3.1]nonan-4-ol (3a) was achieved using an osmium tetroxide mediated oxidation of the known intermediate 6. A pyrrolidine-ring variant of 3a (3-(7-(hydroxymethyl)-6-methyl-6-azabicyclo[3.2.1]octan-1-yl)phenol (5)) was is...
The anti-diabetic activity of the methanolic extract of Uvaria afzelii (Annonaceae) root bark was investigated in normoglycaemic, glucose and alloxan-induced diabetic rats using glibenclamide (5 mg/kg) and normal saline as positive and negative controls respectively. The acute oral toxicity test...
New azafluorenones, 2-aryl-4-(4-hydroxyphenyl)-5H-indeno[1,2-b]pyridin-5-ones, were prepared to evaluate their cytotoxic/anticancer properties, also their inhibitory effects on hCA I and II isoenzymes. Aryl part was changed as [phenyl (H1), 4-methylphenyl (H2), 4-methoxyphenyl (H3), 4-fluorophen...
16-Dehydroprogesterone reductase (16-DHPR) activity was present in cell extracts of Eubacterium sp. strain 144 only when the organism was grown in the presence of steroids containing a Δ16–17 double bond and C-20-ketone. Cells grown with 16-dehydropregnenolone contained 16-DHPR activity but la...
Eubacterium sp. 144 biotransformed 16-dehydroprogesterone by initially hydrating approx 50% to 16α-hydroxyprogesterone. The detection of this reaction was dependent, in part, on the solubility state of 16-dehydroprogesterone and was less extensive when the concentration of methanol was insuffic...
Cetyltrimethylammonium permanganate initiates oxidative opening of the D-ring of 16-dehydroprogesterone in CH2Cl2. The novel steroids 3 and 4 have been isolated and characterized as the major products obtained from oxidative rearrangement of the steroid backbone. The X-ray crystal structure of t...
Novel benzylidenes (chalcones) of the 16-dehydroprogesterone series have been characterized and their antitumor activity against two breast cancer cell lines was evaluated. Benzylidenes exhibit significant antiproliferative effect on cells and inhibit cell growth in hormone-dependent MCF-7 and h...
Using a large sample of transaction-level institutional trading data, we investigate the role of institutional investors in stock market around the terrorist attacks on September 11, 2001 (9/11), a sudden exogenous catastrophic shock to financial markets. We find that institutional investors rem...
ObjectiveTo determine the effects of fluconazole on oral methadone pharmacokinetics and central effects mediated by opioid receptors in dogs.
The reaction of trithiophosphites, P(SR)3 (R = CH3, C2H5 and C6H5 ), with M(CO)5X (M = Mn, Re, X = Cl, Br) yields complexes of the general formula M(CO)4P(SR)3X and M(CO)3[P(SR)3]2X. The geometry of the disubstituted complexes is established from infrared and PMR spectroscopy to be fac-Re(CO)3[P...
Alkyl- and phenyl-substituted borate anion receptors, triphenyl borate (TPB) and trimethyl borate (TMB), are investigated as electrolyte additives in lithium ion batteries (LiFePO4 cathode, 1 M LiPF6 EC-DMC 1:1 electrolyte) at 25 and 60 °C. TPB shows formation of a thick surface/electrolyte int...
Nickel-rich cathode material has received marked attention as an advanced cathode material, however, its inferior surface property limits the achievement of high performance in lithium-ion batteries. We propose the use of a bi-functional additive of triphenyl borate (TPB) for improvement of the ...
Herein we report triphenyl borate as a new catalyst for synthesis of amides by catalytic condensation of carboxylic acids and amines. Our protocol is applicable for synthesis of wide range of amides furnishing excellent yields up to 92%. In addition developed method requires low catalyst loading...
The metabolism of biphenyl in the rat has been studied by using gas chromatographic and mass spectrometric methods. The free and conjugated urinary metabolites were characterized. Eight new metabolites were isolated: a dihydrodiol and two hdroxydihydrodiols were characteristic for the epoxide—d...
The cyclization of 1,3-bis(trimethylsilyloxy)-1,3-butadienes with 3-oxo-bis(methylthio)ketenacetals afforded 3-(methylthio)phenols containing an acyl or ester substituent located at position 2. The cyclization of free 1,3-dicarbonyl dianions with 3-oxo-bis(methylthio)ketenacetals resulted in the...
Nicotinic acid mononucleotide adenylyltransferase (NaMNAT) is an indispensable enzyme for the synthesis of NAD and NAD phosphate. It catalyzes the adenylylation of nicotinic acid mononucleotide (NaMN) to yield nicotinic acid adenine dinucleotide (NaAD). Since NAD(H) and NAD phosphate(H) are esse...
This study was initiated to determine whether the protective effect of nicotinamide (NAM) on high glucose/palmitate (HG/PA)-induced INS-1 beta cell death was due to its role as an anti-oxidant, nicotinamide dinucleotide (NAD+) precursor, or inhibitor of NAD+-consuming enzymes such as poly (ADP-r...
Amyloid-β (Aβ) oligomers have been accepted as major neurotoxic agents in the therapy of Alzheimer’s disease (AD). It has been shown that the activity of nicotinamide adenine dinucleotide (NAD+) is related with the decline of Aβ toxicity in AD. Nicotinamide mononucleotide (NMN), the importan...
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