Synthesis and vasodilator activity of new piperazine derivatives

Regnier, G.; Canevari, R.; Laubie, Michel; Douarec, J. C. Le

doi:10.1021/jm00312a010

Cited by 56 publications

(9 citation statements)

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“…The latter compound was prepared according to a procedure described by Achilefu. 54 Compound 18 was obtained in 76% yield under the experimental conditions described by Regnier et al 55 Alkylation of the phenol oxygen with N-(2-hydroxyethyl)iminodiacetic acid di-t-butyl ester 56 under the Mitsunobu reaction conditions yielded compound 19, which was quantitatively converted into ligand 4a upon treatment with TFA. Compound 5a was prepared in a similar manner except that the initial Mannich reaction was conducted with 2 molar equivalents of iminodiacetic acid di-t-butyl ester and excess formaldehyde, in N-methylmorpholine (NMM).…”

Section: Design and Synthesis Of The Ligandsmentioning

confidence: 99%

Synthesis and characterization of coumarin-based europium complexes and luminescence measurements in aqueous media

et al. 2009

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A series of new ligands suitable for the formation of luminescent lanthanide complexes in water is described. The chelates are designed for analyte labeling and play the role of fluorescent donor in homogeneous time-resolved fluorescence assays using LEDs as a light source for excitation at 370 nm. Ligands are constructed from a coumarin nucleus, for lanthanide sensitization, and different aminomethylenecarboxy moieties are introduced in positions 7 and 5, 6, or 8 of the sensitizer. A reactive spacer arm under biocompatible conditions (maleimide, azide) is introduced at position 3 for ultimate bioconjugation purposes. The synthesis and characterization of the ligands are described, together with the preparation of their corresponding europium complexes. Photophysical properties of the complexes are investigated in water by means of UV-vis and luminescence spectroscopy.

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Section: Design and Synthesis Of The Ligandsmentioning

confidence: 99%

Synthesis and characterization of coumarin-based europium complexes and luminescence measurements in aqueous media

et al. 2009

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“…Piribedil (PD), is an alkoxybenzyl-4-(2-pyrimidinyl) piperazine derivative with vasodilatory activity [30]. Piribedil has proved active in patients with Parkinson's disease, particularly in the control of tremors [31].…”

Section: Trimetazidine Hydrochloride (Tmh) I -[(234-trimethoxyphenyl)mentioning

confidence: 99%

Spectrophotometric determination of some pharmaceutical piperazine derivatives by charge-transfer and ion-pair complexation methods

et al. 2002

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Simple and sensitive spectropliotometric methods are described for the assay of three piperazine derivatives ketoconazole, trimetazidine hydrochloride and piribedil based on cliarge-transfer and ion-pair complexation reactions. The first method is based on the reaction of the basic drug with iodine as o-acceptor in dry 1,2-dichloroethane to form a yellow colour due to the formation of charge-transfer complex showing maximum absorbence at 363, 364 and 359 nm for ketoconazole, trimetazidine hydrochlorid and piribedil, respectively. The second method is based on the reaction of basic drug with bromocresol green (BCG) in dry 1,2- dichloroethane to form a stable yellow coloured complex with maximum absorbance at 407, 408 and 410 nm for ketoconazol, trimetazidine hydrochloride and piribedil, respectively. Beer's law was obeyed for both methods and the relative standard deviations were found to be less than 1%. The two methods can be applied for the analysis of tablets and cream, with no evidence of interference from excipients. A more detailed investigation of the complex was made with respect to its composition association constant and free energy cliange.

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“…1) has become a commonly prescribed antidepressant 2 and piribedil is employed for its dopaminergic action against cognitive pathological deficit. 3 Furthermore, they represent protected forms of catechol moiety, scaffold of catecholamines and also included in the structure of entacapone. 4 This is used in the treatment of Parkinson's disease, as adjuvant to levodopa therapy.…”

Section: Introductionmentioning

confidence: 99%