20850-12-8Relevant academic research and scientific papers
USE OF SPIRO [ IMIDAZOLIDINE-4, 3'-INDOLE] 2, 2', 5' (1H) TRIONES FOR TREATMENT OF CONDITIONS ASSOCIATED WITH VANILLOID RECEPTOR 1
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Page/Page column 18; 24-25, (2008/06/13)
The present invention relates to a new use of spiro-hydantoin derivatives of formula (I), or salts, solvates or solvated salts thereof, as well as to new compounds, a process for their preparation and new intermediates used in the preparation thereof, pha
NEW COMPOUNDS I
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Page/Page column 28-29, (2008/06/13)
The present invention relates to new compounds of formula (I), wherein R1 to R9 and X are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the
Synthesis, modelling, and μ-opioid receptor affinity of N-3(9)-arylpropenyl-N-9(3)-propionyl-3,9-diazabicyclo[3.3.1]nonanes
Pinna,Murineddu,Curzu,Villa,Vianello,Borea,Gessi,Toma,Colombo,Cignarella
, p. 553 - 562 (2007/10/03)
A series of N-3-arylpropenyl-N-9-propionyl-3,9-diazabicyclo[3.3.1]nonanes (1a-g) and of reverted N-3-propionyl-N-9-arylpropenyl isomers (2a-g), as homologues of the previously reported analgesic 3,8-diazabicyclo[3.2.1]octanes (I-II), were synthesized and evaluated for the binding affinity towards opioid receptor subtypes μ, δ and κ. Compounds 1a-g and 2a-g exhibited a strong selective μ-affinity with Ki values in the nanomolar range, which favourably compared with those of I and II. In addition, contrary to the trend observed for DBO-I, II, the μ-affinity of series 2 is markedly higher than that of the isomeric series 1. This aspect was discussed on the basis of the conformational studies performed on DBN which allowed hypotheses on the mode of interaction of these compounds with the μ receptor.
Pyrazolopyrimidine Ribonucleosides as Anticoccidials. 3. Synthesis and Activity of Some Nucleosides of 4-pyrazolopyrimidines
Rideout, Janet L.,Krenitsky, Thomas A.,Chao, Esther Y.,Elion, Gertrude B.,Williams, Raymond B.,Latter, Victoria S.
, p. 1489 - 1494 (2007/10/02)
Ribonucleosides of 4-(alkylthio)-1H-pyrazolopyrimidines have been shown to be useful anticoccidial agents .In that study, the unsaturated 4-allylthio and 4-crotylthio derivatives (19 and 20) were shown to be more active in vivo against Eimeria tenella than their saturated congeners; therefore, some unsaturated (arylalkyl)thio derivatives were synthesized and investigated as anticoccidial agents.The novel compounds in this study (2 to 18) were prepared by the alkylation of 4-mercapto-1-β-D-ribofuranosyl-1H-pyrazolopyrimidine (1), which was prepared by an enzymatic method.The (E)-4-cinnamylthio derivative (2) and the 5'-monophosphate (18) were the most active compounds against E. tenella in vivo.None of the analogues with substituents in the aryl moiety (3 to 13) was more active than 2 in vivo.The geometry about the double bond was important, since the (Z)-4-cinnamylthio derivative (14) was inactive both in vitro and in vivo.The 4-(3-phenylpropynyl)thio and 4-(5-phenyl-2,4-pentadienyl)thio derivatives (15 and 16) were at least as active as 2 in vitro; however, they were less active than 2 in vivo.Compound 2 was effective in vivo against E. tenella, E. necatrix, E. maxima, and E. brunetti; these species of Eimeria were controlled when 2 was given in the diet at levels up to 100 ppm.Infections in vivo due to E. acervulina were controlled by 2 only at about 800 ppm.The broad spectrum of anticoccidial activity shown by 2 represents a significant improvement over the activities reported for related compounds .
