118133-15-6Relevant articles and documents
Synthesis, Biological, and Computational Evaluation of Substituted 1-(2-Methoxyphenyl)-4-(1-phenethylpiperidin-4-yl)piperazines and 1-(2-Methoxyphenyl)-4-[(1-phenethylpiperidin-4-yl)methyl]piperazines as Dopaminergic Ligands
Penji?evi?, Jelena Z.,?ukalovi?, Vladimir V.,Andri?, Deana B.,Rogli?, Goran M.,?o?ki?, Vuki?,Kosti?-Raja?i?, Sla?ana V.
, p. 614 - 626 (2016)
Sixteen new 1-(2-methoxyphenyl)-4-(1-phenethylpiperidin-4-yl)piperazines and 1-(2-methoxyphenyl)-4-[(1-phenethylpiperidin-4-yl)methyl]piperazines were synthesized to be used as probes for mapping the dopamine D2 receptor (D2DAR) arylpiperazine binding site. All compounds were evaluated for their affinity toward D2DAR in an in vitro competitive displacement assay. The most active one was 1-(2-methoxyphenyl)-4-{[1-(3-nitrophenethyl)piperidin-4-yl]methyl}piperazine (25) with an affinity of Ki = 54 nM. Docking analysis was conducted on all herein described compounds, whereas molecular dynamic simulation was performed on ligand 25 to establish its mode of interaction with D2DAR. Two possible docking orientations are proposed; the one with a salt bridge between the piperidine moiety and Asp114 of D2DAR is more stable.
Benzonaphthyrindines compounds and pharmaceutical compositions thereof and its application in pharmacy
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Paragraph 0069; 0070, (2019/01/28)
The invention provides a pyrazolopyrimidine compound shown as a structural formula (I), a pharmaceutical composition taking the pyrazolopyrimidine compound as an active component, a preparation method of the pyrazolopyrimidine compound and the pharmaceutical composition as well as an application of the pyrazolopyrimidine compound and the pharmaceutical composition in preparation of a TRPC6 (Transient Receptor Potential Channel 6) adjustor probe medicine and related medicines for preventing and treating glomerulopathy and myocardial hypertrophy. The pyrazolopyrimidine compound and derivatives provided by the invention can be used to prepare medical preparations in various forms which comprise oral liquids, injections, pulmonary inhalation preparations and transdermal preparations, specifically injections, oral liquids, troches, capsules, granules, aerosols, dry powder inhalation, patches and the like.
ANTIVIRAL ETHERS OF ASPARTATE PROTEASE SUBSTRATE ISOSTERES
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, (2008/06/13)
Antiretroviral compounds (which are effective, for example, against HIV) of the formula I STR1 in which R 1 is an acyl radical lower-alkoxyl-lower-alkanoyl whose lower alkoxy radical is unsubstituted or is substituted by halogen, phenyl, lower alkoxy or a heterocyclic radical selected from piperidinyl, pyrrolidinyl, tetrahydropyranyl, tetrahydrofuranyl, thiazolidinyl, thiazolyl, indolyl or 4H-1-benzopyranyl which is unsubstituted or substituted by oxo, hydroxyl, amine, lower alkyl, lower-alkoxycarbonyl and/or phenyl-lower-alkoxycarbonyl; lower alkanoyl which is unsubstituted or is substituted by one of the said unsubstituted or substituted heterocyclic radicals; arylcarbonyl or heterocyclylcarbonyl which are substituted by heterocyclyl or heterocyclyl-lower-alkyl; phenyl-lower-alkanoyl which is substituted by hydroxyl and lower alkyl; or arylsulfonyl;or the residue of an amino acid which is defined in accordance with the description (and which may be acylated on the amino nitrogen by one of the abovementioned acyl radicals);R 2 and R 3 are in each case cyclohexyl, cyclohexenyl, phenyl, naphthyl or tetrahydronaphthyl which are unsubstituted or substituted by lower alkyl, phenyl, cyanophenyl, phenyl-lower-alkyl, halogen, halo-lower-alkyl, cyano, hydroxyl, lower alkoxy, phenyl-lower-alkoxyl, pyridyl-lower-alkoxy, lower-alkoxy-lower-alkoxy, lower-alkoxycarbonyl-lower-alkoxy, carboxyl-lower-alkoxy, hydroxyl-lower-alkoxy, carbamoyl-lower-alkoxy, cyano-lower-alkoxy, and phenyl-lower-alkanesulfonyl which is unsubstituted or substituted by halogen;R 4 is lower alkyl, cyclohexyl or phenyl; and R 5 is lower alkyl; and n is 1 or 2, or salts thereof, are novel.
