《1-Aryl-3-(4-pyridine-2-ylpiperazin-1-yl)propan-1-one Oximes as Potent Dopamine D4 Receptor Agonists for the Treatment of Erectile Dysfunction》 was written by Kolasa, Teodozyj; Matulenko, Mark A.; Hakeem, Ahmed A.; Patel, Meena V.; Mortell, Kathleen; Bhatia, Pramila; Henry, Rodger; Nakane, Masaki; Hsieh, Gin C.; Terranova, Marc A.; Uchic, Marie E.; Miller, Loan N.; Chang, Renje; Donnelly-Roberts, Diana L.; Namovic, Marian T.; Hollingsworth, Peter R.; Martino, Brenda; El Kouhen, Odile; Marsh, Kennan C.; Wetter, Jill M.; Moreland, Robert B.; Brioni, Jorge D.; Stewart, Andrew O.. Computed Properties of C17H19N5 And the article was included in Journal of Medicinal Chemistry on August 24 ,2006. The article conveys some information:
A new series of dopamine D4 receptor agonists, 1-aryl-3-(4-pyridinepiperazin-1-yl)propanone oximes, was designed through the modification of known dopamine D4 receptor agonist PD 168077. Replacement of the amide group with a methylene-oxime moiety produced compounds with improved stability and efficacy. Structure-activity relationships (SAR) of the aromatic ring linked to the N-4-piperazine ring confirmed the superiority of 2-pyridine as a core for D4 agonist activity. A two-methylene linker between the oxime group and the N-1-piperazine ring displayed the best profile. New dopamine D4 receptor agonists, exemplified by (E)-1-(4-chlorophenyl)-3-(4-pyridin-2-ylpiperazin-1-yl)propan-1-one O-methyloxime(I) (59a) and (E)-1-(3-chloro-4-fluorophenyl)-3-(4-pyridin-2-ylpiperazin-1-yl)propan-1-one O-methyloxime (II) (64a), exhibited favorable pharmacokinetic profiles and showed oral bioavailability in rat and dog. Subsequent evaluation of 59a in the rat penile erection model revealed in vivo activity, comparable in efficacy to apomorphine. Our results suggest that the oximes provide a novel structural linker for 4-arylpiperazine-based D4 agonists, possessing leadlike quality and with potential to develop a new class of potent and selective dopamine D4 receptor agonists. In the experiment, the researchers used many compounds, for example, Abt-724(cas: 70006-24-5Computed Properties of C17H19N5)
Abt-724(cas: 70006-24-5) belongs to piperazines. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines.Computed Properties of C17H19N5
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics