Cowart, Marlon; Latshaw, Steven P.; Bhatia, Pramila; Daanen, Jerome F.; Rohde, Jeffrey; Nelson, Sherry L.; Patel, Meena; Kolasa, Teodozyi; Nakane, Masaki; Uchic, Marie E.; Miller, Loan N.; Terranova, Marc A.; Chang, Renjie; Donnelly-Roberts, Diana L.; Namovic, Marian T.; Hollingsworth, Peter R.; Martino, Brenda R.; Lynch, James J. III; Sullivan, James P.; Hsieh, Gin C.; Moreland, Robert B.; Brioni, Jorge D.; Stewart, Andrew O. published an article in Journal of Medicinal Chemistry. The title of the article was 《Discovery of 2-(4-Pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (ABT-724), a Dopaminergic Agent with a Novel Mode of Action for the Potential Treatment of Erectile Dysfunction》.Category: piperazines The author mentioned the following in the article:
A new class of agents with potential utility for the treatment of erectile dysfunction has been discovered, guided by the hypothesis that selective D4 agonists are erectogenic but devoid of the side effects typically associated with dopaminergic agents. The lead agent 2-(4-pyridin-2-ylpiperazin-1-ylmethyl)-1H-benzimidazole (1, ABT-724) was discovered by optimization of a series of benzimidazole arylpiperazines. This highly selective D4 agonist was found to be very potent and efficacious in vivo, eliciting penile erections in rats at a dose of 0.03 μmol/kg, with a pos. response rate of 77% erectile incidence. Even at high doses, it was devoid of side effects in animal models of central nervous system behaviors, emesis, or nausea. The structure-activity relationship of the parent benzimidazole series leading to 1 is described, with the detailed in vitro and in vivo profiles described. Distinctive structural features were discovered that are associated with D4 selective agonism in this series of analogs. The experimental process involved the reaction of Abt-724(cas: 70006-24-5Category: piperazines)
Abt-724(cas: 70006-24-5) belongs to piperazines. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Category: piperazines
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics