2,5-Diketopiperazines as Potent, Selective, and Orally Bioavailable Oxytocin Antagonists. 2. Synthesis, Chirality, and Pharmacokinetics was written by Borthwick, Alan D.;Davies, Dave E.;Exall, Anne M.;Livermore, David G.;Sollis, Steve L.;Nerozzi, Fabrizio;Allen, Michael J.;Perren, Marion;Shabbir, Shalia S.;Woollard, Patrick M.;Wyatt, Paul G.. And the article was included in Journal of Medicinal Chemistry in 2005.SDS of cas: 27913-99-1 This article mentions the following:
A short stereoselective synthesis of a series of chiral 7-aryl-2,5-diketopiperazines oxytocin antagonists is described. Varying the functionality and substitution pattern of substituents in the 7-aryl ring and varying the chirality of this exocyclic ring have produced potent oxytocin antagonists (pKi > 8.5). SAR and pharmacokinetic profiling of this series of (3R,6R,7R)-2,5-diketopiperazines together with the introduction of an ortho F group in the 7-aryl ring to improve rat pK has culminated in the 2′,4′-difluorophenyldiketopiperazine derivative I, a highly potent oxytocin antagonist against the human oxytocin receptor (pKi = 8.9) that has >1000-fold selectivity over all three vasopressin receptors V1a, V2, and V1b. It has good bioavailability (46%) in the rat and moderate bioavailability (13-31%) in the dog and is more active in vivo in the rat than atosiban (rat DR10 = 0.44 mg/kg iv). In the experiment, the researchers used many compounds, for example, 4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1SDS of cas: 27913-99-1).
4-(4-Methylpiperazin-1-yl)benzaldehyde (cas: 27913-99-1) belongs to piperazine derivatives. Industrial applications of piperazine include the manufacture of plastics, resins, pesticides and brake fluids. Outside the body, piperazine has a remarkable power to dissolve uric acid and producing a soluble urate, but in clinical experience it has not proved equally successful. SDS of cas: 27913-99-1
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics