BACKGROUND Two 99mTc-DTPA attached estrone derivatives were synthesized and their radiopharmaceutical potential was determined using female albino Wistar rats. MATERIALS AND METHODS Two novel radiolabeled estrone derivatives, 99mTc-2,2',2"2"'-(2,2'-(2-(3-methoxy-13-methyl-17-oxo-7, 8, 9, 11, 12, 13, 14, 15, 16, 7-decahydro-6H- cyclopenta[a]phenanthren-2-ylamino)-2- oxoethylazanediyl) bis(etha...

To screen for residues of hKv1.3 important for current block by the phenylalkylamine verapamil, the inactivated-state-reduced H399T mutant was used as a background for mutagenesis studies. This approach was applied mainly to abolish the accumulation in the inactivated blocked state, recovery from which in the wild type is normally slow. Substitution of amino acids in the S6 transmembrane helix ...

A series of indole-ethylamines were tested for their ability to suppress the spontaneous firing of single dorsal raphe serotonergic neurons in the rat. The compounds were all derivatives of either tryptamine or N,N-dimethyltryptamine possessing hydroxy or methoxy substituents on the benzene ring portion of the indole nucleus. Their activity was assessed using quantitative microiontophoresis or ...

BACKGROUND The overproduction of nitric oxide (NO) is known to involve in various inflammatory processes. A methanol extract of the tubers of Ophiopogon japonicus was found to strongly inhibit NO production. The present paper deals with the isolation, structural identification and NO inhibitory effect of five compounds isolated from the MeOH extract of O. japonicus tubers. RESULTS Three new c...

A novel one step regioand stereoselective synthesis of functionalised bicyclo[2.2.2]octenones from readily available aromatic precursors is described. The methodology involved in situ generation of reactive spiroepoxycyclohexadienones and p4sþp2s cycloaddition with methyl vinyl ketone. Study on p-facial alkylation that led to the formation of homobrendane derivatives as a result of stereochemic...

Thirteen polyphenolics were isolated from fresh pods of Caesalpinia pulcherrima using various methods of column chromatography. The structures of these polyphenolics were elucidated as gallic acid (1), methyl gallate (2), 6-O-galloyl-d-glucoside (3), methyl 6-O-galloyl-β-d-glucoside (4), methyl 3,6-di-O-galloyl-α-d-glucopyranoside (5), gentisic acid 5-O-α-d-(6'-O-galloyl)glucopyranoside (6), gu...

The present study evaluated the antioxidant potential of 28 coumarin derivatives, using three antioxidant assays: DPPH inhibition, total reducing power and NO inhibition. Out of the tested compounds, the most active DPPH free radicals scavengers were the coumarin hydrazide derivatives. These substances were also the only ones among the investigated derivatives that exhibited a moderate reducing...

The objective of this investigation was to find a simple method for the production of phenolic rich products and sugar derivatives (biopolyols) via separation of liquefied lingocellulosic materials. Liquefaction of lignocellulosic materials was conducted in methanol at 180 °C for 15 min with the conversion of raw materials at about 75%. After liquefaction, the liquefied products were separated ...

During the investigation of ester derivatives (juvenogens, biochemically activated insect hormonogenic compounds) of biologically active alcohols with potential application in insect pest control, a need for availability of all existing stereoisomers of ethyl N-{2-[4-(2-butanoyloxycyclohexyl)methyl]phenoxy}ethyl carbamate occurred. They were synthesized from their chiral precursors, the corresp...