• DOI:10.1002/CBDV.200590100
• Corpus ID: 94008789

α1‐ and α2‐Adrenoreceptor Antagonist Profiles of 1‐ and 2‐[ω‐(4‐Arylpiperazin‐1‐yl)alkyl]‐1,2,3‐benzotriazoles

@article{Boido20051A,
  title={$\alpha$1‐ and $\alpha$2‐Adrenoreceptor Antagonist Profiles of 1‐ and 2‐[$\omega$‐(4‐Arylpiperazin‐1‐yl)alkyl]‐1,2,3‐benzotriazoles},
  author={Alessandro Boido and Roberta Budriesi and Caterina Canu Boido and Pierfranco Ioan and Emanuela Terranova and Alberto Chiarini and Fabio Sparatore},
  journal={Chemistry \& Biodiversity},
  year={2005},
  volume={2}
}

• A. Boido, R. Budriesi, +4 authors F. Sparatore
• Published 1 October 2005
• Biology, Chemistry
• Chemistry & Biodiversity

A series of pharmacologically interesting 1‐ and 2‐[ω‐(4‐arylpiperazin‐1‐yl)alkyl]‐1,2,3‐benzotriazoles, compounds 1–27, were synthesized (Scheme) and subjected to various biological studies to identify structure–activity relationships (SAR). The new compounds were found to exhibit good non‐selective binding affinity towards the α1‐adrenoreceptor (Table 1). In several cases, high functional antagonism was observed towards the α1A‐, α1B‐, and α1D‐adrenoreceptor subtypes (Table 2). The selectivity for these three subtypes was comparable with or superior to that displayed by the standard drug prazosin. The most‐common selectivity rank order was α1D>α1B>α1A, followed by α1B>α1D>α1A. In functional experiments, antagonism towards the α2‐adrenoreceptor was generally low; however, a few compounds were endowed with significant antagonist properties (pA2 values of up to 7.87).