51299-27-5

Upstream product

• 107-04-0 1-Bromo-2-chloroethane 
• 1011-15-0 1-(o-fluorophenyl)piperazine 

Downstream Products

• 1334582-06-7 C₂₀H₂₂FN₅ 
• 1334582-16-9 C₂₀H₂₂FN₅ 
• 1262048-35-0 1-{2-[4-(2-fluorophenyl)piperazin-1-yl]ethyl}-2-pyridin-3-yl-1H-benzimidazole 

Relevant academic research and scientific papers

Synthesis and biological activity of new 1,4-benzodioxan-arylpiperazine derivatives. Further validation of a pharmacophore model for α1-adrenoceptor antagonists

A series of WB4101 (1)-related benzodioxanes (2-17) have been synthesized by replacing the phenoxyethyl moiety of 1 with a N-alkyl piperazine bearing a cyclic substituent (a substituted or unsubstituted phenyl group, a pyridine or pyridazinone ring, a furoyl moiety) at the second nitrogen atom. The binding profile of these compounds has been assessed by radioligand receptor binding assay at α1- and α2-adrenoceptors, in comparison to prazosin and rauwolscine, respectively. Moreover, structure-activity relationships have been derived for compounds 2-17 based on their fitting to a pharmacophore model for α1-adrenoceptor antagonists recently proposed by our research group. In a parallel way, the same compounds have been used to further test the predictive power and statistical significance of the model itself. The accuracy of the results obtained also in this case revealed the robustness of the calculated pharmacophore model and led to the identification of the molecular structural moieties which are thought to contribute to the biological activity. Copyright

Synthesis of a novel series of 4-arylpiperazinyl derivatives linked to a 2-(Pyridin-3-yl)-1H-benzimidazole as new delavirdine analogues

The synthesis of a series of substituted arylpiperazines linked to a 2-(pyridin-3-yl)-1H-benzo[d] imidazole scaffold through an alkylic linker is reported. The novel 1-(2-(4-arylpiperazin-1-yl) alkyl)-2-(pyridin-3-yl)-1H- benzimidazole derivatives are structurally related to the anti-HIV-1 drug Delavirdine and belong to the bis(heteroaryl)piperazines family (BHAPs), a well known HIV-1 reverse transcriptase inhibitors group.

Compounds specific for the human alpha1d adrenergic receptor and uses thereof

This invention is directed towards a method of inhibiting activation of a human α1d adrenergic receptor which comprises contacting the receptor with a compound so as to inhibit activation of the receptor, wherein the compound binds selectively to a human ald adrenergic receptor. This invention provides for a compound which binds selectively to a human α1d adrenergic receptor. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier. This invention further provides for a method of treating a subject afflicted with a disease which is susceptible to treatment by antagonism of the human α1d adrenergic receptor which comprises administering to the subject an amount of the above defined compounds effective to treat the disease.

Synthesis of new 1,2,3-benzotriazin-4-one-arylpiperazine derivatives as 5-HT(1A) serotonin receptor ligands

A series of novel 1,2,3-benzotriazin-4-one derivatives was prepared and evaluated as ligands for 5-HT receptors. Radioligand binding assays proved that the majority of the novel compounds behaved as good to excellent ligands at the 5-HT(1A) receptor, some of which were selective with respect 5-HT(2A) and 5-HT(2C) receptors. Six analogues (1a, 2a, 2b, 2c, 2e and 2i) were selected and further evaluated for their binding affinities on D1, D2 dopaminergic and α1-, α2-adrenergic receptors. A o-OCH3 derivative (2e) bound at 5-HT(1A) sites with subnanomolar affinity (IC50=0.059 nM) and shows high selectivity over all considered receptors and may offer a new lead for the development of therapeutically efficacious agents. Copyright (C) 2000 Elsevier Science Ltd.