35288-13-2Relevant academic research and scientific papers
4-Imidazole derivatives of benzyl and restricted benzyl sulfonamides, sulfamides, ureas, carbamates, and amides and their use
-
, (2008/06/13)
Compounds of formula I are useful in treating diseases prevented by or ameliorated with α1A agonists. Also disclosed are α1A agonist compositions and a method of activating α1 adrenoceptors in a mammal.
Hydrocarbon humps in the marine environment: Synthesis, toxicity, and aqueous solubility of monoaromatic compounds
Smith, Emma,Wraige, Emma,Donkin, Peter,Rowland, Steven
, p. 2428 - 2432 (2007/10/03)
A recent study has shown that some monoaromatic hydrocarbon constituents of the so-called unresolved complex mixtures (UCMs) or gas chromatographic humps, which are widespread in the marine environment, are toxic to the mussel Mytilus edulis. Here we describe the synthesis and toxicological assessment of 6-cyclohexyltetralin, 7-cyclohexyl-1-methyltetralin, and 7-cyclohexyl-1-n-propyltetralin, which contain structural features consistent with some monoaromatic UCM hydrocarbons. The compounds were all toxic to M. edulis when measured in the assay used previously to determine the toxicity of a monoaromatic UCM. The aqueous solubilities of the hydrocarbons in fresh and seawater at different temperatures were determined and found to range from about 10 to 110 μg/L (10-60 μg/L in seawater at 15°C). Further studies of the aromatic UCM composition of a wide range of oils and oil residues are required to determine whether such alkylated compounds as 7-cyclohexyl-1-methyltetralin and 7-cyclohexyl-1-n-propyltetralin or their analogues are widespread in oils. If these aromatic compounds prove to be important in UCMs, toxicity experiments should be conducted with other biological end points and monitoring studies of pollutant hydrocarbons should probably include measurement of aromatic UCM hydrocarbons.
Phosphonic acid compounds, their production and use
-
, (2008/06/13)
The present invention relates to a compound of the general formula (I): STR1 wherein ring A is a benzene ring that may be substituted; Y is a divalent group as a constituent member of ring B forming a 5- to 8-membered ring; Q1 is a group of the formula --X--P(O)(OR1)(OR2) wherein X is a bond or a divalent group; R1 and R2, identical or different, are hydrogen or a lower alkyl, or may be combined together to form a ring; Q2 is hydrogen, a hydrocarbon group that may be substituted or a heterocyclic group that may be substituted; and the group of the formula --CON(Q1)(Q2) is connected to the a- or b-position carbon atom, or a salt thereof, which is useful as prophylactic and therapeutic agents of various metabolic bone diseases such as osteoporosis.
ON THE QUANTITATIVE RELATIONS BETWEEN STRUCTURE AND ANTIAGGREGATION ACTIVITY OF ω-ARYL-ω-OXOALKANOIC ACIDS
Kuchar, Miroslav,Brunova, Bohumila,Grimova, Jaroslava,Rejholec, Vaclav,Cepelak, Vaclav
, p. 2617 - 2625 (2007/10/02)
A series of ω-aryl-ω-oxoalkanoic acids, I-IV, has been prepared and investigated for dissociation constants in 80percent methylcellosolve, retention characteristics in thin-layer partition chromatography and partition coefficients P in the system octanol-water.Also evaluated were their anti-inflammatory efficacy and inhibitory effect on the platelet aggregation induced by collagen.Analysing the relations between structure and antiaggregation effect, we obtained a non-linear, quadratic dependence of this effect on lipophilicity, the optimum being at log P = 3.The antiaggregation effect increased with shortening the chain between the carbonyl and the carboxyl, and with increasing acidity.It was also diminished by the presence of a methyl group on the interlinking chain.To assess the role of lipophilicity we used the RM values of partition chromatography.The relation between anti-inflammatory efficacy and structure was assessed only qualitatively.In this aspect, too, the nature of the chain between the carbonyl and carboxyl proved to have a marked influence.The anti-inflammatory activity proved considerably enhanced by the presence of another aromatic ring in ω-oxoalkanoic acids derived from biphenyl.
A new non-steroidal anti-inflammatory analgesic: γ-oxo(1,1'-biphenyl)-4-butanoic acid (fenbufen)
Child,Osterberg,Sloboda,Tomcufcik
, p. 695 - 702 (2007/10/02)
100 analogs of γ-oxo(1,1'-biphenyl)-4-butanoic acid (fenbufen) were prepared and tested using the carrageenin, polyarthritis, and UV erythema anti-inflammatory tests and the 2-phenyl-1,4-benzoquinone writhing and inflamed paw pressure analgesic tests. Only three retained the same full spectrum of activity as fenbufen: dl-4-(4-biphenyl)-4-hydroxybutyric acid, dl-4-(4-biphenylyl)-1,4-butanediol, and 4-biphenylacetic acid. Fenbufen had the same spectrum of activity as acetylsalicylic acid (ASA), phenylbutazone, and indomethacin in the five tests. In addition, dose-response derived potencies show fenbufen more potent than ASA and at least as potent as phenylbutazone in all five tests.
Fenbufen, a new anti inflammatory analgesic: synthesis and structure activity relationships of analogs
Child,Osterberg,Sloboda,Tomcufcik
, p. 466 - 476 (2007/10/05)
100 analogs of fenbufen were prepared and tested using the carrageenan, polyarthritis, and UV erythema anti inflammatory tests and the 2 phenyl 1,4 benzoquinone writhing and inflamed paw pressure analgesic tests. Only 3 retained the same full spectrum of activity as fenbufen: dl 4 (4 biphenylyl) 4 hydroxybutyric acid, dl 4 (4 biphenylyl) 1,4 butanediol, and 4 biphenylacetic acid. Fenbufen had the same spectrum of activity as aspirin, phenylbutazone, and indomethacin in the 5 tests. In addition, dose response derived potencies show fenbufen more potent than aspirin and at least as potent as phenylbutazone in all 5 tests. Two related compounds were generally similar.
