39496-87-2Relevant academic research and scientific papers
N-(2-(SUBSTITUTED-NAPHTH-1-YL)ETHYL) SUBSTITUTED AMIDE COMPOUND, PREPARATION AND USES THEREOF
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Paragraph 0063; 0064, (2020/06/04)
The present disclosure relates to an N-(substituted naphthyl-ethyl) substituted amide compound and uses thereof serving as a melatonin receptor agonist and 5-HT2C receptor antagonist, and specifically relates to the compound of formula (I) or a
A novel type of retinoic acid receptor antagonist: Synthesis and structure-activity relationships of heterocyclic ring-containing benzoic acid derivatives
Yoshimura,Nagai,Hibi,Kikuchi,Abe,Hida,Higashi,Yamanaka
, p. 3163 - 3173 (2007/10/02)
A new series of heterocyclic ring-containing benzoic acids was prepared, and the binding affinity and antagonism of its members against all-trans- retinoic acid were evaluated by in vitro assay systems using human promyelocytic leukemia (HL-60) cells. Structure-activity relationships indicated that both an N-substituted pyrrole or pyrazole (1-position) and a hydrophobic region, with these linked by a ring system, were indispensable for effective antagonism. Among the compounds evaluated, optimal antagonism was exhibited by 4-[4,5,7,8,9,10-hexahydro-7,7,10,-10-tetramethyl-1-(3- pyridylmethyl)anthra[1,2-b]pyrrol-3-yl]benzoic acid (31), 4-[4,5,7,8,9,10- hexahydro-7,7,10,10-tetramethyl-1-(3-pyridylmethyl)-5-thiaanthra[1,2- b]pyrrol-3-yl]benzoic acid (40), and 4-[4,5,7,8,9,10-hexahydro-7,7,10,10- tetramethyl-1-(3-pyridylmethyl)anthra[2,1-d]pyrazol-3-yl]benzoic acid (55), all of which possess a 3-pyridylmethyl group at the five-membered ring nitrogen atom.
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.
