Design, synthesis and biological evaluation of naphthalimidebased fluorescent probes for α1-adrenergic receptors

Discovery of Quinazoline-Based Fluorescent Probes to α1-Adrenergic Receptors

“…Among all chemotypes, quinazoline compounds, including prazosin, terazosin, doxazosin, and alfuzosin, are the most clinically effective α 1 -AR antagonists (Scheme ) . In our previous study, a pharmacophore model based on quinazoline derivatives that contribute many effective α 1 -AR antagonists was well built, and the proposed interaction model of quinazoline-based antagonists with α 1 -ARs was well developed. − It was found that there is a bulky space around the piperazine group to accommodate the fluorophore moiety, which does not influence the affinity of antagonists to receptors. Therefore, in the current research, we chose the quinazoline moiety as the pharmacophore to generate fluorescent probes for selectively binding with α 1 -ARs.…”