Synthesis and structure-activity relationships of novel arylpiperazines as potent antagonists of 浼?-adrenoceptor was written by Silva, Renata Oliveira;de Oliveira, Andressa Souza;Nunes Lemes, Lais Flavia;de Camargo Nascente, Luciana;Coelho do Nascimento Nogueira, Patricia;Silveira, Edilberto R.;Brand, Guilherme D.;Vistoli, Giulio;Cilia, Antonio;Poggesi, Elena;Buccioni, Michela;Marucci, Gabriella;Bolognesi, Maria Laura;Romeiro, Luiz Antonio Soares. And the article was included in European Journal of Medicinal Chemistry in 2016.Electric Literature of C9H11BrO This article mentions the following:
Arylpiperazines 2-11 were synthesized, and their biol. profiles at 浼?-adrenergic receptors (浼?-ARs) assessed by binding assays in CHO cells expressing human cloned subtypes and by functional experiments in isolated rat vas deferens (浼?A), spleen (浼?B), and aorta (浼?D). Modifications at the 1,3-benzodioxole and Ph phamacophoric units resulted in the identification of a number of potent compounds (moderately selective with respect to the 浼?b-AR), in binding experiments Notably, compound 7 (LDT451) showed a subnanomolar pKi of 9.41 towards 浼?a-AR. An encouragingly lower 浼?B-potency was a general trend for all the series of compounds, which showed 浼?A/D over 浼?B selectivity in functional assays. If adequately optimized, such peculiar selectivity could have relevance for a potential LUTS/BPH therapeutic application. In the experiment, the researchers used many compounds, for example, 1-(2-Bromoethyl)-4-methoxybenzene (cas: 14425-64-0Electric Literature 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. In the pharmaceutical industry organo bromine derivatives are used as sedatives, vasodilators, antiseptic agents, and anticancer agents.Electric Literature of C9H11BrO
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary