Targeting Serotonin 2A and Adrenergic α1 Receptors for Ocular Antihypertensive Agents: Discovery of 3,4-Dihydropyrazino[1,2-b]indazol-1(2H)-one Derivatives was written by Furlotti, Guido;Alisi, Maria Alessandra;Cazzolla, Nicola;Ceccacci, Francesca;Garrone, Beatrice;Gasperi, Tecla;La Bella, Angela;Leonelli, Francesca;Loreto, Maria Antonietta;Magaro, Gabriele;Mangano, Giorgina;Bettolo, Rinaldo Marini;Masini, Emanuela;Miceli, Martina;Migneco, Luisa Maria;Vitiello, Marco. And the article was included in ChemMedChem in 2018.Computed Properties of C9H11BrO This article mentions the following:
Glaucoma affects millions of people worldwide and causes optic nerve damage and blindness. The elevation of the intraocular pressure (IOP) is the main risk factor associated with this pathol., and decreasing IOP is the key therapeutic target of current pharmacol. treatments. As potential ocular hypotensive agents, the authors studied compounds that act on two receptors (serotonin 2A and adrenergic α1) linked to the regulation of aqueous humor dynamics. Herein, the design, synthesis, and pharmacol. profiling of a series of novel bicyclic and tricyclic N2-alkyl-indazole-amide derivatives is described. This study identified a 3,4-dihydropyrazino[1,2-b]indazol-1(2H)-one derivative I with potent serotonin 2A receptor antagonism, >100-fold selectivity over other serotonin subtype receptors, and high affinity for the α1 receptor. Moreover, upon local administration, this compound showed superior ocular hypotensive action in vivo relative to the clin. used reference compound timolol. In the experiment, the researchers used many compounds, for example, 1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0Computed Properties of C9H11BrO).
1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0) belongs to organobromine compounds. Most of the natural organobromine compounds are produced by marine organisms, and several brominated metabolites with antibacterial, antitumor, antiviral, and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Computed Properties of C9H11BrO
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary