Design, synthesis and pharmacological profile of novel dopamine D2 receptor ligands

1‐Cinnamyl‐4‐(2‐methoxyphenyl)piperazines: Synthesis, Binding Properties, and Docking to Dopamine (D2) and Serotonin (5‐HT1A) Receptors

“…They are also a part of numerous high-affinity ligands for different G-protein coupled receptors [14]. In D 2 -, 5-HT 2A -, and a 1 -functional tests most of them behaves as antagonist [13,15,16] although few exceptions are reported in the literature [17]. The recently published trans-1-[(2-phenylcyclopropyl)methyl]-4-arylpiperazines [18] K i values represent the means of three independent experiments, done in triplicate using eight ligand concentrations (1.0 nM -0.1 mM), according to the methods described in Experimental (section 4); S.E.M.…”

Development and validation of a LC-MS/MS method with electrospray ionization for determination of LASSBio-579 in rat plasma

“…Two of the compounds obtained were LASSBio-581 (1-[1-(4-chloro-phenyl)-1H- [1,2,3]triazol-4-ylmethyl]-4-phenyl-piperazine) and LASSBio-579 (1-[1-(4-chloro-phenyl)-1H-pyrazol-4-ylmethyl]-4-phenylpiperazine) (Fig. 1) [3].…”

Synthesis and evaluation of 1-alkyl-4-phenyl-[1,2,3]-triazole derivatives as antimycobacterial agent

“…In particular, when the reaction occurs between alkyl or aryl azides and terminal acetylenes, [1,2,3]-triazoles are obtained. [9][10][11][12][13][14][15][16][17][18][19][20][21] If the cycloaddition is thermally conduced, a 1:1 mixture of the 1,4 and 1,5-regioisomers of triazole is usually obtained. Various attempts to control the regioselectivity without much success were reported until the discovery of the copper(I)-catalyzed reaction in 2002, which exclusively yields the 1,4-disubstituted-[1,2,3]-triazole.…”

“…1 H NMR spectra were obtained on a Varian Mercury Plus 400-MHz instrument, with tetramethylsilane (TMS) as the internal standard. 13 C NMR spectra were recorded on a Varian Mercury Plus 100-MHz spectrometer. The chemical shifts are given as delta (δ) values and the coupling constants (J) in Hertz (Hz).…”